PI103http://www.medchemexpress.com/PI-103.html is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
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2014年8月17日星期日
TGX-221 from medchemexpress
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TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β .
TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β .
TG100-115 from medchemexpress
TG100–115 is a PI3K γ and -δ inhibitor (IC50 = 83 and 235 nM, respectively)
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AS-605240 from medchemexpress
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AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) (IC50 = 8 nM). AS-605240 displays 30-fold selectivity over PI3Kδ and PI3Kβ and 7.5-fold selectivity over PI3Kα.
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) (IC50 = 8 nM). AS-605240 displays 30-fold selectivity over PI3Kδ and PI3Kβ and 7.5-fold selectivity over PI3Kα.
LY294002 from medchemexpress
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LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively.
LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively.
Navitoclax from medchemexpress
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Navitoclax is a novel, oral BH3 mimetic, potently inhibits multiple antiapoptotic Bcl-2 family proteins.
Navitoclax is a novel, oral BH3 mimetic, potently inhibits multiple antiapoptotic Bcl-2 family proteins.
Triapine from medchemexpress
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3-AP and 3-AP-Me activated the cellular stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinases, and inhibition of JNK activity antagonized the cytotoxic effect of both compounds. 3-AP and 3-AP-Me induce apoptosis via ER stress [1]. Triapine abolishes olaparib-induced BRCA1 and Rad51 foci, and disrupts the BRCA1 interaction with the Mre11-Rad50-Nbs1 (MRN) complex in BRCA1 wild-type EOC cells. triapine inhibits cyclin-dependent kinase (CDK) activity and blocks olaparib-induced CtIP phosphorylation through Chk1 activation. triapine abrogates etoposide-induced CtIP phosphorylation and DSB resection as evidenced by marked attenuation of RPA32 phosphorylation [2].
Triapine(NSC663249; OCX191; PAN-811) is a ribonucleotide reductase inhibitor, has been extensively evaluated in clinical trials in the last decade; CDK inhibtor.
3-AP and 3-AP-Me activated the cellular stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinases, and inhibition of JNK activity antagonized the cytotoxic effect of both compounds. 3-AP and 3-AP-Me induce apoptosis via ER stress [1]. Triapine abolishes olaparib-induced BRCA1 and Rad51 foci, and disrupts the BRCA1 interaction with the Mre11-Rad50-Nbs1 (MRN) complex in BRCA1 wild-type EOC cells. triapine inhibits cyclin-dependent kinase (CDK) activity and blocks olaparib-induced CtIP phosphorylation through Chk1 activation. triapine abrogates etoposide-induced CtIP phosphorylation and DSB resection as evidenced by marked attenuation of RPA32 phosphorylation [2].
Triapine(NSC663249; OCX191; PAN-811) is a ribonucleotide reductase inhibitor, has been extensively evaluated in clinical trials in the last decade; CDK inhibtor.
WYE-125132 from medchemexpress
WYE-125132 is a highly potent, ATP-competitive and specific mTOR kinase inhibitor with an IC50 of 0.19 nM, highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.
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A 922500 from medchemexpress
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A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor.
in vitro: A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM [1].
in vivo: Zucker fatty rats and diet-induced dyslipidemic hamsters were dosed orally with A-922500 (0.03, 0.3, and 3-mg/kg), a potent and selective DGAT-1 inhibitor, for 14 days. Serum triglycerides were significantly reduced by the 3 mg/kg dose of the DGAT-1 inhibitor in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%) [1]. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice [2]. The potent and selective DGAT-1 inhibitorA-922500 (0.03, 0.3 and 3 mg/kg, p.o.), dose-dependently attenuated the maximal postprandial rise in serum triglyceride concentrations in all species tested. At the highest dose of DGAT-1 inhibitor, the postprandial triglyceride response was abolished
A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor.
in vitro: A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM [1].
in vivo: Zucker fatty rats and diet-induced dyslipidemic hamsters were dosed orally with A-922500 (0.03, 0.3, and 3-mg/kg), a potent and selective DGAT-1 inhibitor, for 14 days. Serum triglycerides were significantly reduced by the 3 mg/kg dose of the DGAT-1 inhibitor in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%) [1]. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice [2]. The potent and selective DGAT-1 inhibitorA-922500 (0.03, 0.3 and 3 mg/kg, p.o.), dose-dependently attenuated the maximal postprandial rise in serum triglyceride concentrations in all species tested. At the highest dose of DGAT-1 inhibitor, the postprandial triglyceride response was abolished
MK-0591 from medchemexpress
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Varenicline(CP 526555; Champix; Chantix) is a prescription medication used to treat smoking addiction. As a partial agonist it both reduces cravings for and decreases the pleasurable effects of cigarettes and other tobacco products. Through these mechanisms Varenicline(CP 526555; Champix; Chantix) can assist some patients to quit smoking.
Varenicline(CP 526555; Champix; Chantix) is a prescription medication used to treat smoking addiction. As a partial agonist it both reduces cravings for and decreases the pleasurable effects of cigarettes and other tobacco products. Through these mechanisms Varenicline(CP 526555; Champix; Chantix) can assist some patients to quit smoking.
E 2012 from medchemexpress
E 2012 is γ-secretase inhibitor.
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PAP-1 from medchemexpress
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PAP-1 is selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. Effective orally or intraperitoneally. 5-(4-Phenoxybutoxy)psoralen has 23-fold selectivity for Kv1.3 over Kv1.5, and 33-125-fold selectivity over other Kv1 family channels. In treatment of multiple sclerosis
PAP-1 is selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. Effective orally or intraperitoneally. 5-(4-Phenoxybutoxy)psoralen has 23-fold selectivity for Kv1.3 over Kv1.5, and 33-125-fold selectivity over other Kv1 family channels. In treatment of multiple sclerosis
SCH 563705 from medchemexpress
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SCH 563705, a potent CXCR2 and CXCR1 antagonist, has therapeutic potential for targeting CXCR2/CXCR1 in human arthritides.
SCH 563705, a potent CXCR2 and CXCR1 antagonist, has therapeutic potential for targeting CXCR2/CXCR1 in human arthritides.
Ko 143 from medchemexpress
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Ko 143 is potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM). Ko 143 displays > 200-fold selectivity over P-gp and MRP-1 transporters. Ko 143 increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance.
Ko 143 is potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM). Ko 143 displays > 200-fold selectivity over P-gp and MRP-1 transporters. Ko 143 increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance.
PKI-587 inhibitors from medchemexpress
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PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 μM for PI3K-α and mTOR, respectively.
TWS119 from medchemexpress
TWS119 is inhibitor of glycogen synthase kinase-3β (IC50 = 30 nM). TWS119 induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs).
To identify the differentially over-expressed genes associated with β-catenin accumulation in nuclei of hepatocellular carcinoma (HCC) cells. METHODS: Differentially expressed genes were identified in radiation-induced B6C3 F1 mouse HCC cells by mRNA differential display, Northern blot and RT-PCR, respectively. Total glutathione-s-transferase (GST) activity was measured by GST activity assay and β-catenin localization was detected with immunostaining in radiation-induced mouse HCC cells and in HepG2 cell lines. RESULTS: Two up-regulated genes, glutamine synthetase and glutathione-s-transferase M3 (GSTM3), were identified in radiation-induced mouse HCC cells. Influence of β-catenin accumulation in nuclei of HCC cells on up-regulation of GSTM3 mRNA was investigated. The nearby upstream domain of GSTM3 contained the β-catenin/Tcf-Lef consensus binding site sequences [5'-(A/T)(A/T) CAAAG-3'], and the total GST activity ratio was considerably higher in B6C3F1 mouse HCC cells with β-catenin accumulation in nuclei of HCC cells than in those without β-catenin accumulation (0.353 ± 0.117 vs. 0.071 ± 0.064, P < 0.001). The TWS119 (a distinct GSK-3β inhibitor)-induced total GST activity was significantly higher in HepG2 cells with β-catenin accumulation than in those without β-catenin accumulation in nuclei of HCC cells. Additionally, the GSTM3 mRNA level was significantly higher at 24 h than at 12 h in TWS119-treated HepG2 cells. CONCLUSION: β-catenin accumulation increases GST activity in nuclei of HCC cells, and GSTM3 may be a novel target gene of the β-catenin/Tcf-Lef complex.
2 . Zeng FY, Dong H, Cui J, Liu L, Chen T.Glycogen synthase kinase 3 regulates PAX3-FKHR-mediated cell proliferation in human alveolar rhabdomyosarcoma cells.Biochem Biophys Res Commun. 2010 Jan 1;391(1):1049-55. Epub 2009 Dec 6.
To identify the differentially over-expressed genes associated with β-catenin accumulation in nuclei of hepatocellular carcinoma (HCC) cells. METHODS: Differentially expressed genes were identified in radiation-induced B6C3 F1 mouse HCC cells by mRNA differential display, Northern blot and RT-PCR, respectively. Total glutathione-s-transferase (GST) activity was measured by GST activity assay and β-catenin localization was detected with immunostaining in radiation-induced mouse HCC cells and in HepG2 cell lines. RESULTS: Two up-regulated genes, glutamine synthetase and glutathione-s-transferase M3 (GSTM3), were identified in radiation-induced mouse HCC cells. Influence of β-catenin accumulation in nuclei of HCC cells on up-regulation of GSTM3 mRNA was investigated. The nearby upstream domain of GSTM3 contained the β-catenin/Tcf-Lef consensus binding site sequences [5'-(A/T)(A/T) CAAAG-3'], and the total GST activity ratio was considerably higher in B6C3F1 mouse HCC cells with β-catenin accumulation in nuclei of HCC cells than in those without β-catenin accumulation (0.353 ± 0.117 vs. 0.071 ± 0.064, P < 0.001). The TWS119 (a distinct GSK-3β inhibitor)-induced total GST activity was significantly higher in HepG2 cells with β-catenin accumulation than in those without β-catenin accumulation in nuclei of HCC cells. Additionally, the GSTM3 mRNA level was significantly higher at 24 h than at 12 h in TWS119-treated HepG2 cells. CONCLUSION: β-catenin accumulation increases GST activity in nuclei of HCC cells, and GSTM3 may be a novel target gene of the β-catenin/Tcf-Lef complex.
2 . Zeng FY, Dong H, Cui J, Liu L, Chen T.Glycogen synthase kinase 3 regulates PAX3-FKHR-mediated cell proliferation in human alveolar rhabdomyosarcoma cells.Biochem Biophys Res Commun. 2010 Jan 1;391(1):1049-55. Epub 2009 Dec 6.
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2014年8月11日星期一
SB-705498 inhibitors from medchemexpress
SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1. SB-705498 potently inhibits capsaicin-induced activation of human TRPV1 expressed in 1321N1 cells or HEK293 cells with apparent pKi of 7.5 or 7.6, respectively. Coapplication of 100 nM SB-705498 rapidly, completely and reversibly inhibits hTRPV1 expressed in HEK293 cells. Compared with placebo, SB-705498 reduced the area of capsaicin-evoked flare (P=0.0047). The heat pain threshold on non-sensitised skin was elevated following SB-705498 (estimated difference from placebo [95% confidence intervals]: 1.3 degrees C [0.07,2.53], P=0.019). Following capsaicin sensitisation, the heat pain threshold and tolerance were similar between SB-705498 and placebo. However, SB-705498 increased heat pain tolerance at the site of UVB-evoked inflammation (estimated difference from placebo: 0.93 degrees C [0.25,1.6], P=0.0054). The magnitude of the pharmacodynamic effects of SB-705498 appeared to be related to plasma concentration. These results indicate that SB-705498, at a clinically safe and well-tolerated dose, has target-specific pharmacodynamic activity in humans. These data provide the first clinical evidence that a TRPV1 antagonist may alleviate pain and hyperalgesia associated with inflammation and tissue injury.
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TWS119 inhibitors from medchemexpress
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TWS119 is inhibitor of glycogen synthase kinase-3β (IC50 = 30 nM). TWS119 induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs).
TWS119 is inhibitor of glycogen synthase kinase-3β (IC50 = 30 nM). TWS119 induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs).
BIX-01294 inhibitors from medchemexpress
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BIX-01294, a diazepin-quinazolinamine derivative, is a selective inhibitor of G9a histone methyl transferase (G9a HMTase) that impairs G9a HMTase and generation of H3K9me2 in vitro. In its inhibition of the histone lysine methyltransferases, BIX-01294 does not compete with cofactor S-adenosyl-methionine. G9a HMTase regulates gene expression including one of the pluripotency genes Oct4. It is reported that BIX-01294 enhances reprogramming efficiency of neural progenitor cells to the same levels as when four transcription factors (Oct4, Klf4, Sox2 and c-Myc) were introduced to somatic cells for generation of induced pluripotent stem cells. BIX-01294 and valproic acid, a histone deacetylase (HDAC) inhibitor, may replace the requirement for ectopic OCT4 (POU5F1) and cMyc respectively in pluripotent stem cell induction (iPS) recipes.
BIX-01294, a diazepin-quinazolinamine derivative, is a selective inhibitor of G9a histone methyl transferase (G9a HMTase) that impairs G9a HMTase and generation of H3K9me2 in vitro. In its inhibition of the histone lysine methyltransferases, BIX-01294 does not compete with cofactor S-adenosyl-methionine. G9a HMTase regulates gene expression including one of the pluripotency genes Oct4. It is reported that BIX-01294 enhances reprogramming efficiency of neural progenitor cells to the same levels as when four transcription factors (Oct4, Klf4, Sox2 and c-Myc) were introduced to somatic cells for generation of induced pluripotent stem cells. BIX-01294 and valproic acid, a histone deacetylase (HDAC) inhibitor, may replace the requirement for ectopic OCT4 (POU5F1) and cMyc respectively in pluripotent stem cell induction (iPS) recipes.
GW 5074 inhibitors from medchemexpress
GW 5074 is a potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC50 = 9 nM). GW 5074 displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm.
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MK 2206 inhibitors from medchemexpress
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MK-2206 2Hcl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed.
MK-2206 2Hcl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed.
TH-302 inhibitors from medchemexpress
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TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM, demonstrates 270-fold enhanced cytotoxicity under hypoxia versus their potency under aerobic conditions, stable to cytochrome P450 metabolism.
TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM, demonstrates 270-fold enhanced cytotoxicity under hypoxia versus their potency under aerobic conditions, stable to cytochrome P450 metabolism.
SRT 1720 inhibitors from medchemexpress
SRT 1720 is a SIRT1 activator. Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. SRT 1720 is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC1.5 = 0.16 versus 46.2 μM, respectively). SRT 1720 is useful for treatment of type 2 diabetes.
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ARRY-380 inhibitors from medchemexpress
ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. ErbB-2 inhibitor ARRY-380 selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. ErbB-2 is overexpressed in a variety of cancers and plays an important role in cellular proliferation and differentiation.
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GSK1904529A inhibitors from medchemexpress
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GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.
GSK1904529A, which potently inhibits IGF-IR (IC50= 27 nmol/L) and IR (IC50= 25 nmol/L) activities in vitro and in vivo, is a promising candidate for therapeutic use in solid and hematologic cancers.
GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.
GSK1904529A, which potently inhibits IGF-IR (IC50= 27 nmol/L) and IR (IC50= 25 nmol/L) activities in vitro and in vivo, is a promising candidate for therapeutic use in solid and hematologic cancers.
CGP 57380 inhibitors from medchemexpress
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CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 (IC50 = 2.2 μM) with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 (IC50 = 2.2 μM) with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
IC50 value: 2.2 uM
Target: Mnk1
in vitro: Inhibition of MNK1 activity by a specific inhibitor (CGP57380) enhanced differentiation of HL60 and 32D cells, further suggesting a role for MNK1 in the myeloid differentiation. CGP 57380 effectively inhibits eIF4E phosphorylation (IC50 = 3 μM) by MNK1 in 293 human embryonic kidney cells and serves as a useful tool in studying Mnk1-mediated cellular signaling. CGP 57380 is an inhibitor of ARK-2, BRSK2, ChoK, Dyrk3, Lck, Mnk2 and SGK.
Target: Mnk1
in vitro: Inhibition of MNK1 activity by a specific inhibitor (CGP57380) enhanced differentiation of HL60 and 32D cells, further suggesting a role for MNK1 in the myeloid differentiation. CGP 57380 effectively inhibits eIF4E phosphorylation (IC50 = 3 μM) by MNK1 in 293 human embryonic kidney cells and serves as a useful tool in studying Mnk1-mediated cellular signaling. CGP 57380 is an inhibitor of ARK-2, BRSK2, ChoK, Dyrk3, Lck, Mnk2 and SGK.
SU5416 inhibitors from medchemexpress
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR.
SU5416 (Semaxinib), a VEGF receptor inhibitor and an aryl hydrocarbon receptor (AHR) agonist, represents a new alternative for immunomodulation. SU5416 went as far as Phase III clinical trials as an anticancer agent, putatively because of its activity as a VEGFR-2 inhibitor. SU5416 has biologic activity in patients with refractory acute myeloid leukemia or myelodysplastic syndromes. SU5416 inhibits tumor vascularization and growth of multiple tumor types.
Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR.
SU5416 (Semaxinib), a VEGF receptor inhibitor and an aryl hydrocarbon receptor (AHR) agonist, represents a new alternative for immunomodulation. SU5416 went as far as Phase III clinical trials as an anticancer agent, putatively because of its activity as a VEGFR-2 inhibitor. SU5416 has biologic activity in patients with refractory acute myeloid leukemia or myelodysplastic syndromes. SU5416 inhibits tumor vascularization and growth of multiple tumor types.
VX-745 inhibitors from medchemexpress
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
VX-745 is highly potent and selective p38α inhibitor (IC50 = 10 nM). VX-745 also blocks TNFα production in LPS-stimulated HWB in vitro (IC50 = 177 nM). VX-745 displays 1000-fold selectivity over closely related kinases, including ERK1, MK2 and JNK1-3. VX-745 is a lead anti-inflammatory candidate, p38 MAPK inhibitor (IC50=10 nM) for the treatment of Rheumatoid arthritis (RA).
VX-745 is highly potent and selective p38α inhibitor (IC50 = 10 nM). VX-745 also blocks TNFα production in LPS-stimulated HWB in vitro (IC50 = 177 nM). VX-745 displays 1000-fold selectivity over closely related kinases, including ERK1, MK2 and JNK1-3. VX-745 is a lead anti-inflammatory candidate, p38 MAPK inhibitor (IC50=10 nM) for the treatment of Rheumatoid arthritis (RA).
PD173074 inhibitors from medchemexpress
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PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM, ~1000-fold selective for FGFR1 than PDGFR and c-Src.PD173074 is a potent ATP-competitive, reversible FGFR and VEGFR inhibitor with IC50 of 5, 21.5 and ~100 nM for FGFR3, FGFR1 and VEGFR2, respectively.
PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM, ~1000-fold selective for FGFR1 than PDGFR and c-Src.PD173074 is a potent ATP-competitive, reversible FGFR and VEGFR inhibitor with IC50 of 5, 21.5 and ~100 nM for FGFR3, FGFR1 and VEGFR2, respectively.
GSK2126458 from medchemexpress
GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.
GSK2126458 (GSK212) is a highly potent PI3K and mTOR inhibitor with an app Ki of 19 pM for PI3K.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
GSK2126458 (GSK212) is a highly potent PI3K and mTOR inhibitor with an app Ki of 19 pM for PI3K.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
GSK-923295 from medchemexpress
GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183.Novel drug candidate for the treatment of cancer, GSK-923295(
1088965-37-0 ), is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E, (CENP-E).
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
2014年8月7日星期四
medchemexpress supply high quality inhibitors
United States of America, 6 August 2014: Research Chemicals and other biochemicals are one of the key elements for conducting various kinds of experiments. Moreover, most chemicals are known for their hazardous nature and any differences or duplicates could turn to be highly dangerous. Hence, it is more than important to get these chemicals from reputed and well-known suppliers. The market has various brands and many of them have grown reliable over the years and decades. One company which has been offering these chemicals as well as biochemicals for a long time is MedChemExpress (MCE). The products include life science reagents, APIs, reference compounds, and other natural components which are used at laboratory as well as scientific experiments.
The company is operated and supervised by an experienced as well as enthusiastic team of technical and customer support teams. The members have years of experience in the Life Science industry. The team is known to pay a lot of attention on purity, stability as well as activity of compounds. Their expertise and experience makes them competent enough to be a trustworthy partner. They supply various chemicals such as the enzyme inhibitors, AEE788, or the ZD-4054. In order to offer quality products, the company has implemented a quality control policy which helps in catering to quality chemicals test data.
Moreover, the company offers its services in the field of preparing biologically active molecules which are both synthetically as well as structurally diverse in use. The volumes offered by the company ranges from a few milligrams to kilograms as per the needs of the customers. Lastly, the rich experience in the field of customized chemical synthesis that ensures timely delivery for diversified compounds for meeting the clients having different requirements. Customers having any kind of queries or suggestions can get in touch with the company’s representatives through the contact options mentioned on the website. Moreover, they can also call on their helpline numbers or drop in an email at the mentioned contact numbers and email addresses.
The website features all the relevant information regarding the products and services the company has on offer. Moreover, the site offers various kinds of resources for chemicals, calculators, as well as other technical details to help their customers understand about the right usage of the chemicals they purchase. Customers would also be pleased to know that the company uses some of the most advanced packing materials to ensure that the products are stored and delivered in the right conditions to the customers.
MedChemExpress:
MedChemExpress offers various kinds of chemicals as well as biochemical along with technical services in the field of research as well as scientific activities. To know more about their products and services, customers can browse their website or download the catalog from the website.
Read Original Article - See more at: http://www.prnutshell.com/pressreleases/6655/medchemexpress-offers-its-range-of-research-chemicals-and-biochemicals#sthash.T5EbjUBj.dpuf
Read Original Article - See more at: http://www.prnutshell.com/pressreleases/6655/medchemexpress-offers-its-range-of-research-chemicals-and-biochemicals#sthash.T5EbjUBj.dpuf
2014年8月4日星期一
PF-5274857
PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
BMS-833923 inhibitors
Description:
IC50 Value: 6-35 nM [1]
BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity. SMO antagonist BMS-833923 inhibits the sonic hedgehog (SHH) pathway protein SMO, which may result in a suppression of the SHH signaling pathway.
in vitro: In vitro, BMS-833923 inhibits the expression of downstream effectors in the HH pathway (GLI1 and PTCH1) in cell lines that express wild-type SMO and those which express activated mutant forms of SMO (IC50values of 6-35 nM). In FACS-based binding assays, BMS-833923 inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM [1].
in vivo: Pharmacodynamic studies show that BMS-833923 robustly inhibits HH pathway activity with along duration of action after a single oral dose in medulloblastoma and pancreatic carcinoma xenograft models. The pharmacodynamic effects of BMS-833923 observed in these models translate into tumor growth inhibition at well-tolerated doses [1].
Clinical trial: Dasatinib Combo With Smoothened (SMO) Antagonist (BMS-833923). Phase 2
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
IC50 Value: 6-35 nM [1]
BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity. SMO antagonist BMS-833923 inhibits the sonic hedgehog (SHH) pathway protein SMO, which may result in a suppression of the SHH signaling pathway.
in vitro: In vitro, BMS-833923 inhibits the expression of downstream effectors in the HH pathway (GLI1 and PTCH1) in cell lines that express wild-type SMO and those which express activated mutant forms of SMO (IC50values of 6-35 nM). In FACS-based binding assays, BMS-833923 inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM [1].
in vivo: Pharmacodynamic studies show that BMS-833923 robustly inhibits HH pathway activity with along duration of action after a single oral dose in medulloblastoma and pancreatic carcinoma xenograft models. The pharmacodynamic effects of BMS-833923 observed in these models translate into tumor growth inhibition at well-tolerated doses [1].
Clinical trial: Dasatinib Combo With Smoothened (SMO) Antagonist (BMS-833923). Phase 2
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
PF-04449913 inhibitors
PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor.
IC50 value: 5 nM [1]
Target: smoothened
PF-04449913, a Smoothened inhibitor was identified possessing excellent potency and physical properties that translate to an attractive predicted human pharmacokinetic profile. PF-04449913 was advanced to in vivo tumor growth inhibition studies, preclinical safety studies, and ultimately to human clinical trials. These results will be reported in separate disclosures.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
IC50 value: 5 nM [1]
Target: smoothened
PF-04449913, a Smoothened inhibitor was identified possessing excellent potency and physical properties that translate to an attractive predicted human pharmacokinetic profile. PF-04449913 was advanced to in vivo tumor growth inhibition studies, preclinical safety studies, and ultimately to human clinical trials. These results will be reported in separate disclosures.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
LDE225 inhibitors
LDE225 (NVP-LDE225; Erismodegib) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.
IC50 value: 1.3 nM/2.5 nM (Hh signaling Mouse/Human) [1]
Target: Smoothened
in vitro: LDE225 inhibits TM3 luciferized cell line with 0.6 nM and 8 nM, at the presence of 1 nM and 25 nM Hh agonist Ag1.5, respectively [1].
in vivo: LDE225 is highly bound to mouse, rat, and human plasma proteins (>99%) and moderately bound to dog and monkey plasma proteins (77 and 85%, respectively). LDE225 has high permeability (90.8% in man) in the PAMPA assay. LDE225 shows good oral bioavailability ranging from 69 to 102% in preclinical species when dosed in solution. LDE225 is a weak base with a measured pKa of 4.20 and exhibits relatively poor aqueous solubility. LDE225 demonstrates dose-related antitumor activity. At a dose of 5 mg/kg/day qd, LDE225 significantly inhibits tumor growth, corresponding to a T/C value of 33%. When dosed at 10 and 20 mg/kg/day qd, LDE225 gives rise to 51 and 83% regression, respectively. Gli1 mRNA inhibition correlates with tumor and plasma exposure of LDE225. LDE225 successfully penetrates the blood?brain barrier in tumor-bearing animals and results in tumor growth inhibition after 4 days of treatment [1]. LDE225 significantly reduces the tumor volume by 95.7% in Rip1-Tag2 mice. LDE225 prolongs survival in Rip1Tag2 mice. LDE225 decreases expression of stromal markers in the LDE225-treated mice [2].
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
IC50 value: 1.3 nM/2.5 nM (Hh signaling Mouse/Human) [1]
Target: Smoothened
in vitro: LDE225 inhibits TM3 luciferized cell line with 0.6 nM and 8 nM, at the presence of 1 nM and 25 nM Hh agonist Ag1.5, respectively [1].
in vivo: LDE225 is highly bound to mouse, rat, and human plasma proteins (>99%) and moderately bound to dog and monkey plasma proteins (77 and 85%, respectively). LDE225 has high permeability (90.8% in man) in the PAMPA assay. LDE225 shows good oral bioavailability ranging from 69 to 102% in preclinical species when dosed in solution. LDE225 is a weak base with a measured pKa of 4.20 and exhibits relatively poor aqueous solubility. LDE225 demonstrates dose-related antitumor activity. At a dose of 5 mg/kg/day qd, LDE225 significantly inhibits tumor growth, corresponding to a T/C value of 33%. When dosed at 10 and 20 mg/kg/day qd, LDE225 gives rise to 51 and 83% regression, respectively. Gli1 mRNA inhibition correlates with tumor and plasma exposure of LDE225. LDE225 successfully penetrates the blood?brain barrier in tumor-bearing animals and results in tumor growth inhibition after 4 days of treatment [1]. LDE225 significantly reduces the tumor volume by 95.7% in Rip1-Tag2 mice. LDE225 prolongs survival in Rip1Tag2 mice. LDE225 decreases expression of stromal markers in the LDE225-treated mice [2].
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
A-803467 inhibitors
A 803467 is a selective Nav1.8 sodium channel blocker and analgesic. A 803467 blocks Nav1.8 with an IC50 of 8 nM and is over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7. A 803467 dose-dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain models.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
PF-543 inhibitors
PF-543 is a novel cell-permeant inhibitor of SphK1. PF-543 inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. PF-543 is the most potent inhibitor of SphK1 described to date and it will be useful for dissecting specific roles of SphK1-driven S1P signalling.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
K145 inhibitors
K145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 μM , while no inhibition of SphK1 at concentrations up to 10 μM.
IC50 value: 4.3 uM [1]
Target: SphK2
in vitro: K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30±0.06 uM , while no inhibition of SphK1 at concentrations up to 10 uM was observed. Lineweaver-Burk analysis revealed a Ki of 6.4±0.7 uM for SphK2 and indicated that K145 is a substrate competitive inhibitor (with sphingosine). K145 accumulates in U937 cells, suppresses the S1P level, and inhibits SphK2. K145 also exhibited inhibitory effects on the growth of U937 cells as well as apoptotic effects in U937 cells, and that these effects may be through the inhibition of down-stream ERK and Akt signaling pathways [1].
in vivo: K145 also significantly inhibited the growth of U937 tumors in nude mice by both intraperitoneal and oral administration, thus demonstrating its in vivo efficacy as a potential lead anticancer agent [2].
IC50 value: 4.3 uM [1]
Target: SphK2
in vitro: K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30±0.06 uM , while no inhibition of SphK1 at concentrations up to 10 uM was observed. Lineweaver-Burk analysis revealed a Ki of 6.4±0.7 uM for SphK2 and indicated that K145 is a substrate competitive inhibitor (with sphingosine). K145 accumulates in U937 cells, suppresses the S1P level, and inhibits SphK2. K145 also exhibited inhibitory effects on the growth of U937 cells as well as apoptotic effects in U937 cells, and that these effects may be through the inhibition of down-stream ERK and Akt signaling pathways [1].
in vivo: K145 also significantly inhibited the growth of U937 tumors in nude mice by both intraperitoneal and oral administration, thus demonstrating its in vivo efficacy as a potential lead anticancer agent [2].
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
ABC294640 inbihitors
ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. Upon administration, ABC294640 competitively binds to and inhibits SK2, thereby preventing the phosphorylation of the pro-apoptotic amino alcohol sphingosine to sphingosine 1-phosphate (S1P), the lipid mediator that is pro-survival and critical for immunomodulation. This may eventually lead to the induction of apoptosis and may result in an inhibition of cell proliferation in cancer cells overexpressing SK2. SK2 and its isoenzyme SK1 are overexpressed in numerous cancer cell types.<http://www.medchemexpress.com/Targets/SPHK.html>
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
high quality TG 100572 inhibitors from medchemexpress
TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
high quality TG 100801 from medchemexpress
TG 100801 is currently in a clinical trial as a first in class, VEGFr2 targeting, topically applied compound for the treatment of AMD. The formation of new blood vessels (angiogenesis), blood vessel leakage, and inflammation contribute to the progression of the eye disease, age-related macular degeneration (AMD), which is the leading cause of irreversible, severe loss of vision in people 55 years of age and older in the developed world. TG100801 is a new drug that inhibits ocular angiogenesis, vascular leak, and inflammation in laboratory studies, and may have great utility in the treatment of diseases such as AMD.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Saracatinib|medchemexpress
Saracatinib (AZD0530) is a selective, oral Src inhibitor that has demonstrated antitumour activity in preclinical studies. Methods This open-label, dose-escalation, phase I study evaluated the safety and tolerability of saracatinib in Japanese patients with advanced solid tumours (clinicaltrials.gov NCT00704366). Patients received continuous once-daily oral dosing with saracatinib starting 7 days after a single dose in ascending dose cohorts until dose-limiting toxicity (DLT) or disease progression. Pharmacokinetics and efficacy were also evaluated. Results A total of 12 patients received saracatinib at doses of 50 (n?=?3), 125 (n?=?6), and 175 mg (n?=?3). Median durations of exposure were 65, 44, and 16 days in the 50, 125, and 175 mg cohorts, respectively. The most common adverse events were diarrhoea (67?%), nausea (67?%), decreased appetite (58?%), lymphopenia (50?%) and pyrexia (50?%). The most common grade ≥3 adverse events were leukopenia, lymphopenia, neutropenia, and haemoglobin decreased (all 17?%). DLTs occurred in two patients, both in the 175 mg cohort: grade 3 aspartate aminotransferase increased with grade 3 gamma-glutamyltransferase increased (n?=?1); and grade 3 hypoxia (n?=?1). Following a single dose, saracatinib median t(max) across the doses was 2-4 h, and thereafter plasma concentrations declined in a biphasic manner, with mean terminal half-life of approximately 45 h. Geometric mean saracatinib exposures were 0.8-2.1 times greater than those reported in Caucasian patients. The best response was stable disease (50 mg, n?=?2; 125 mg, n?=?1). Conclusions Saracatinib was tolerated in Japanese patients with advanced solid tumours at doses up to 125 mg.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
2014年8月1日星期五
Progesterone
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Progesterone is a C-21 steroid hormone involved in the female menstrual cycle, pregnancy and embryogenesis of humans and other species.
Progesterone also known as P4 (pregn-4-ene-3,20-dione) is a C-21 steroid hormone involved in the female menstrual cycle, pregnancy (supports gestation) and embryogenesis of humans and other species. Progesterone belongs to a class of hormones called progestogens, and is the major naturally occurring human progestogen.
The route of administration impacts the effect of the drug. Given orally, progesterone has a wide person-to-person variability in absorption andbioavailability while synthetic progestins are rapidly absorbed with a longer half-life than progesterone and maintain stable levels in the blood. Progesterone does not dissolve in water and is poorly absorbed when taken orally unless micronized in oil. Products are often sold as capsules containing micronised progesterone in oil. Progesterone can also be administered through vaginal or rectal suppositories or pessaries, transdermally through a gel or cream, or via injection (though the latter has a short half-life requiring daily administration). Transdermal "natural progesterone" products made with Progesterone USP do not require a prescription. Some of these products also contain "wild yam extract" derived from Dioscorea villosa, but there is no evidence that the human body can convert its active ingredient (diosgenin, the plant steroid that is chemically converted to produce progesterone industrially) into progesterone.
Progesterone is a C-21 steroid hormone involved in the female menstrual cycle, pregnancy and embryogenesis of humans and other species.
Progesterone also known as P4 (pregn-4-ene-3,20-dione) is a C-21 steroid hormone involved in the female menstrual cycle, pregnancy (supports gestation) and embryogenesis of humans and other species. Progesterone belongs to a class of hormones called progestogens, and is the major naturally occurring human progestogen.
The route of administration impacts the effect of the drug. Given orally, progesterone has a wide person-to-person variability in absorption andbioavailability while synthetic progestins are rapidly absorbed with a longer half-life than progesterone and maintain stable levels in the blood. Progesterone does not dissolve in water and is poorly absorbed when taken orally unless micronized in oil. Products are often sold as capsules containing micronised progesterone in oil. Progesterone can also be administered through vaginal or rectal suppositories or pessaries, transdermally through a gel or cream, or via injection (though the latter has a short half-life requiring daily administration). Transdermal "natural progesterone" products made with Progesterone USP do not require a prescription. Some of these products also contain "wild yam extract" derived from Dioscorea villosa, but there is no evidence that the human body can convert its active ingredient (diosgenin, the plant steroid that is chemically converted to produce progesterone industrially) into progesterone.
Drospirenone
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Drospirenone(Dihydrospirorenone) is a synthetic progestin that is an analog to spironolactone.
Target: Progesterone Receptor
Drospirenone is a novel progestin under clinical development that is similar to the natural hormone progesterone, combining potent progestogenic with antimineralocorticoid and antiandrogenic activities. drospirenone was devoid of glucocorticoid activity. Both progestins did not show any antiglucocorticoid action. Furthermore, drospirenone and progesterone both showed considerable antimineralocorticoid activity and weak mineralocorticoid activity [1]. the pharmacological profile of drospirenone is more closely related to that of the natural hormone progesterone than is that of any other synthetic progestogen in use today. Therefore, drospirenone is anticipated to give rise to a number of additional health benefits both for users of oral contraceptives and hormone replacement therapy recipients [2]. The combination of 17beta-estradiol and drospirenone has a positive effect on BMD and a potentially beneficial effect on lipids. Although endometrial thickness increased slightly, the safety of the endometrium was assured, as no cases of hyperplasia or cancer occurred [3].
Clinical indications: Acne; Dysmenorrhea; Endometriosis; Female contraception; Folic acid deficiency; Premenstrual syndrome
Drospirenone(Dihydrospirorenone) is a synthetic progestin that is an analog to spironolactone.
Target: Progesterone Receptor
Drospirenone is a novel progestin under clinical development that is similar to the natural hormone progesterone, combining potent progestogenic with antimineralocorticoid and antiandrogenic activities. drospirenone was devoid of glucocorticoid activity. Both progestins did not show any antiglucocorticoid action. Furthermore, drospirenone and progesterone both showed considerable antimineralocorticoid activity and weak mineralocorticoid activity [1]. the pharmacological profile of drospirenone is more closely related to that of the natural hormone progesterone than is that of any other synthetic progestogen in use today. Therefore, drospirenone is anticipated to give rise to a number of additional health benefits both for users of oral contraceptives and hormone replacement therapy recipients [2]. The combination of 17beta-estradiol and drospirenone has a positive effect on BMD and a potentially beneficial effect on lipids. Although endometrial thickness increased slightly, the safety of the endometrium was assured, as no cases of hyperplasia or cancer occurred [3].
Clinical indications: Acne; Dysmenorrhea; Endometriosis; Female contraception; Folic acid deficiency; Premenstrual syndrome
Dienogest
Dienogest(STS-557) is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis.
Target: progesterone receptor agonist
Dienogest is an orally active synthetic progesterone (or progestin). It is available for use as an oral contraceptive in combination with ethinylestradiol. It has antiandrogenic activity and as a result can improve androgenic symptoms. It is a non-ethinylated progestin which is structurally related to testosterone [1].
Complete sperm suppression was observed in rats sacrificed either 60 or 90 days after dienogest (DNG)+ testosterone undecanoate (TU) administration, for two injections at 45-day interval. The neutral α-glucosidase activity in these treated rats remained in the normal range. Germ cell loss due to apoptosis was frequently observed both after 60 or 90 days of combination treatment. Significant decline in serum gonadotropin and testosterone, both serum and intratesticular levels, were observed in the treated rats. Following stoppage of treatment (given at 45-day interval) after two (0 and 45 days) or three injections (0, 45 and 90 days), complete restoration of spermatogenesis was observed by 120 and 165 days, respectively [2].
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Target: progesterone receptor agonist
Dienogest is an orally active synthetic progesterone (or progestin). It is available for use as an oral contraceptive in combination with ethinylestradiol. It has antiandrogenic activity and as a result can improve androgenic symptoms. It is a non-ethinylated progestin which is structurally related to testosterone [1].
Complete sperm suppression was observed in rats sacrificed either 60 or 90 days after dienogest (DNG)+ testosterone undecanoate (TU) administration, for two injections at 45-day interval. The neutral α-glucosidase activity in these treated rats remained in the normal range. Germ cell loss due to apoptosis was frequently observed both after 60 or 90 days of combination treatment. Significant decline in serum gonadotropin and testosterone, both serum and intratesticular levels, were observed in the treated rats. Following stoppage of treatment (given at 45-day interval) after two (0 and 45 days) or three injections (0, 45 and 90 days), complete restoration of spermatogenesis was observed by 120 and 165 days, respectively [2].
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Ulipristal acetate
Ulipristal acetate(CDB2914) is a novel selective progesterone receptor modulator (SPRM) for the treatment of benign gynecological conditions such as uterine myoma.
IC50 value:
Target: progesterone receptor
Ulipristal acetate is used as an emergency contraceptive in women. A single dose of 30 mg ulipristal acetate has recently been proposed for the emergency contraception use up to 120 h of unprotected intercourse with similar side effect profiles as levonorgestrel.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
IC50 value:
Target: progesterone receptor
Ulipristal acetate is used as an emergency contraceptive in women. A single dose of 30 mg ulipristal acetate has recently been proposed for the emergency contraception use up to 120 h of unprotected intercourse with similar side effect profiles as levonorgestrel.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Tanaproget
Tanaproget is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins. Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives.
in vitro: In T47D cells, TNPR induces alkaline phosphatase activity with an EC(50) value of 0.1 nm, comparable with potent steroidal progestins such as medroxyprogesterone acetate (MPA) and trimegestone (TMG), albeit with a reduced efficacy ( approximately 60%). In a mammalian two-hybrid assay to measure PR agonist-induced interaction between steroid receptor co-activator-1 and PR, TNPR showed similar potency (EC(50) value of 0.02 nm) and efficacy to MPA and TMG [1].
in vivo: TNPR effectively down-regulated MMP expression in vitro and induced significant reduction of lesions in mice with disease established by tissues from endometriosis patients [2]. The maximum concentration (C(max)) of tanaproget occurred approximately 2 to 3 h after administration. The elimination half-life (t(1/2)) ranged from 12 to 30 h, and the oral clearance was approximately 70 L/h. The pharmacokinetics of tanaproget was not noticeably altered with a high-fat meal [3].
Toxicity: All doses of tanaproget decreased cervical mucus scores (using a modified Insler method), indicating poor production and poor quality of cervical mucus. The most frequent treatment-emergent adverse events were vaginal bleeding/spotting, abdominal cramping and vomiting; their incidence was not dose related and most events were mild [3].
Clinical trial: N/A
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
in vitro: In T47D cells, TNPR induces alkaline phosphatase activity with an EC(50) value of 0.1 nm, comparable with potent steroidal progestins such as medroxyprogesterone acetate (MPA) and trimegestone (TMG), albeit with a reduced efficacy ( approximately 60%). In a mammalian two-hybrid assay to measure PR agonist-induced interaction between steroid receptor co-activator-1 and PR, TNPR showed similar potency (EC(50) value of 0.02 nm) and efficacy to MPA and TMG [1].
in vivo: TNPR effectively down-regulated MMP expression in vitro and induced significant reduction of lesions in mice with disease established by tissues from endometriosis patients [2]. The maximum concentration (C(max)) of tanaproget occurred approximately 2 to 3 h after administration. The elimination half-life (t(1/2)) ranged from 12 to 30 h, and the oral clearance was approximately 70 L/h. The pharmacokinetics of tanaproget was not noticeably altered with a high-fat meal [3].
Toxicity: All doses of tanaproget decreased cervical mucus scores (using a modified Insler method), indicating poor production and poor quality of cervical mucus. The most frequent treatment-emergent adverse events were vaginal bleeding/spotting, abdominal cramping and vomiting; their incidence was not dose related and most events were mild [3].
Clinical trial: N/A
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Levomefolic acid
Levomefolic acid (5-MTHF) is the natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions. Levomefolic acid has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers. Levomefolic acid (5-MTHF) has the prominent antioxidant activity. A high dose of 5-MTHF or folic acid does not influence Natural killer (NK) cell function in vitro.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Mifepristone
Mifepristone is a synthetic steroid compound used as a pharmaceutical. It is a progesterone receptor antagonist used as an abortifacient in the first months of pregnancy, and in smaller doses as an emergency contraceptive. Mifepristone is also a powerful glucocorticoid receptor antagonist, and has occasionally been used in refractory Cushing's Syndrome.
in vitro: Mifepristone had no effect onHeLa cell proliferation inhibition rate during 24 and 48 hours (p > 0.05). Mifepristone at low concentrations (< or = 10 micromol/l) combined withcisplatin can significantly enhance the inhibitory effect of cisplatin on HeLa cell line [2]. The effect of mifepristone on cytotoxicity of cisplatin could be mediated, at least partially, by an increase of intracellularcisplatin accumulation, but not by changes in Bcl-2/Bax gene relation expression in CaSki cells [3].
in vivo: Mifepristone administration did not alter food intake or weight during the 4-day regimen, nor were there drug-dependent differences in BEL or BCL on withdrawal day. Although mifepristone produced no significant changes in behavior of EtOH-na?ve animals, pretreatment withmifepristone (40 mg/kg) significantly reduced the severity of EtOH withdrawal [4].
Clinical trial: Mifepristone 10 or 5 mg for 6 Months to Treat Uterine Fibroids. Phase 3
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
in vitro: Mifepristone had no effect onHeLa cell proliferation inhibition rate during 24 and 48 hours (p > 0.05). Mifepristone at low concentrations (< or = 10 micromol/l) combined withcisplatin can significantly enhance the inhibitory effect of cisplatin on HeLa cell line [2]. The effect of mifepristone on cytotoxicity of cisplatin could be mediated, at least partially, by an increase of intracellularcisplatin accumulation, but not by changes in Bcl-2/Bax gene relation expression in CaSki cells [3].
in vivo: Mifepristone administration did not alter food intake or weight during the 4-day regimen, nor were there drug-dependent differences in BEL or BCL on withdrawal day. Although mifepristone produced no significant changes in behavior of EtOH-na?ve animals, pretreatment withmifepristone (40 mg/kg) significantly reduced the severity of EtOH withdrawal [4].
Clinical trial: Mifepristone 10 or 5 mg for 6 Months to Treat Uterine Fibroids. Phase 3
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
Nestoron from medchemexpress
Nestoron(ST1435; Elcometrine) is a 19-norprogesterone derivative and steroidal progestin which is used as a hormonal contraceptive; a high-affinity agonist of the progesterone receptor.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
MedChemexpress (MCE) provides a wide range of research chemicals and biochemicals including novel life-science reagents, reference compounds, APIs and Natural compounds for laboratory and scientific use. MCE has an enthusiastic, energetic and friendly Technical and Customer Support team with years of experience in the Life Science industry. MCE pay great attention on the purity, stability and activity of the compounds, esp. You can rely on us to be a competent and trustworthy partner.
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