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Genz-123346 is a glucosylceramide synthase inhibitor with potential anticancer activity. Exposure of cells to Genz-123346 and to other GCS inhibitors at non-toxic concentrations can enhance the killing of tumor cells by cytotoxic anti-cancer agents. Genz-123346 and a few other GCS inhibitors are substrates for multi-drug resistance efflux pumps such as P-gp (ABCB1, gP-170). In cell lines selected to over-express P-gp or which endogenously express P-gp, chemosensitization by Genz-123346 was primarily due to the effects on P-gp function.

June 21, 2017

prudect name : Genz-123346 is a glucosylceramide synthase inhibitor with potential anticancer activity. Exposure of cells to Genz-123346 and to other GCS inhibitors at non-toxic concentrations can enhance the killing…

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GSK1059615 is a dual inhibitor of PI3K¦Á/¦Â/¦Ä/¦Ã (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. IC50 value: 0.4 nM/0.6 nM/2 nM/5 nM(PI3K¦Á/¦Â/¦Ä/¦Ã); 12 nM (mTOR)

prudect name : GSK1059615 is a dual inhibitor of PI3K¦Á/¦Â/¦Ä/¦Ã (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. IC50 value: 0.4 nM/0.6 nM/2…

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GSK2578215A is a potent and highly selective LRRK2 inhibitor; exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant. IC50 value: ~10 nM(wt-LRRK2; LRRK2 G2019S)

prudect name : GSK2578215A is a potent and highly selective LRRK2 inhibitor; exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant. IC50 value: ~10 nM(wt-LRRK2;…

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GSK-1292263 administrated at a single dose of 3-30 mg/kg in the absence of nutrients correlates with increased levels of circulating gastrointestinal peptides, including glucagon-like peptide 1 (GLP-1), gastric inhibitory polypeptide (GIP), peptide YY (PYY) and glucagon in male Sprague-Dawley rats, the increase is enhanced following administration of glucose in the oral glucose tolerance test (OGTT). GSK-129226 significant increases in the peak insulin response and insulin AUC(0-15 min) of 30-60% compared with values in the vehicle control cohort in the intravenous glucose tolerance test in rats, this insulin upregulation correlated with a significant increase in the glucose disposal rate. GSK-1292263 is associated with a statistically significant increase in insulin immunoreactivity in pancreatic sections in a 6-week study performed in Zucker diabetic fatty rats, compared with insulin immunoreactivity in samples obtained from rats receiving vehicle control. GSK-1292263 administrated at dose of 10 or 30 mg/kg or vehicle control at 2 hours prior to insulin infusion in hyperinsulinemic-euglycemic clamps stimulates glucagon secretion without increasing blood glucose levels Sprague-Dawley rats.

prudect name : GSK-1292263 administrated at a single dose of 3-30 mg/kg in the absence of nutrients correlates with increased levels of circulating gastrointestinal peptides, including glucagon-like peptide 1 (GLP-1),…

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GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

prudect name : GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.GSK 429286 A Synonyms: CAS NO: 864082-47-3Molecular Formula: C21H16F4N4O2Molecular Weight:…

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GW9662 is a selective PPAR antagonist for PPAR¦Ã with IC50 of 3.3 nM, with at least 100 to 1000-fold functional selectivity in cells with PPAR¦Ã versus PPAR¦Á and PPAR¦Ä.

prudect name : GW9662 is a selective PPAR antagonist for PPAR¦Ã with IC50 of 3.3 nM, with at least 100 to 1000-fold functional selectivity in cells with PPAR¦Ã versus PPAR¦Á…

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prudect name : Growth hormone releasing peptide;GHRP-6Synonyms: GHRP-6CAS NO: 87616-84-0Molecular Formula: C46H56N12O6Molecular Weight: 873.01Purity: 98%

prudect name : Growth hormone releasing peptide;GHRP-6 Synonyms: GHRP-6CAS NO: 87616-84-0Molecular Formula: C46H56N12O6Molecular Weight: 873.01Purity: 98% minSolubility: Storage: -20°C P-22077 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18516696

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Chemical Name:1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride

prudect name : Chemical Name:1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochlorideGBR 12935 dihydrochloride Synonyms: CAS NO: 76778-22-8Molecular Formula: C28H34N2O.2(HCl)Molecular Weight: 487.50Purity: 98% minSolubility: In DMSOStorage: −20°C R7227 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18516691

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GW3965 recruits the steroid receptor coactivator 1 to human LXR¦Á with EC50 of 125 nM in a cell-free ligand-sensing assay. GW3965 shows a potent antagonistic activity against hLXR¦Á and hLXR¦Â in cell-based assays with EC50 of 190 nM and 30 nM, respectively. Besides, GW3965 also sows excellent selectivity over other nuclear receptors.

prudect name : GW3965 recruits the steroid receptor coactivator 1 to human LXR¦Á with EC50 of 125 nM in a cell-free ligand-sensing assay. GW3965 shows a potent antagonistic activity against…

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GKT137831 is a novel and specific dual Nox1/Nox4 inhibitor with Ki of 140¡À40 nM and 110¡À30 nM; a potent inhibitor of fibrosis and hepatocyte apoptosis.

prudect name : GKT137831 is a novel and specific dual Nox1/Nox4 inhibitor with Ki of 140¡À40 nM and 110¡À30 nM; a potent inhibitor of fibrosis and hepatocyte apoptosis.GSK-137831 Synonyms: CAS…

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