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G007-LK displays high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice.

June 21, 2017

prudect name : G007-LK displays high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50…

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GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22¡À0.1 uM (Wild type Abl).

prudect name : GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22¡À0.1 uM (Wild type Abl).GNF-5;GNF…

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GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate.

prudect name : GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate.GS-7340(Tenofovir alafenamide) Synonyms: CAS NO: 379270-37-8Molecular…

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GSK-503 is a potent EZH2 inhibitor with potential anticancer activity.

prudect name : GSK-503 is a potent EZH2 inhibitor with potential anticancer activity.GSK-503;GSK503 Synonyms: CAS NO: 1346572-63-1Molecular Formula: C31H38N6O2Molecular Weight: 526.67Purity: 98% minSolubility: In DMSOStorage: -20°C ABR 215062 References PubMed…

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SC-203877;5-[3-Methoxy-4-(4-methoxy-benzyloxy)-benzyl]-pyrimidine-2,4-diamine

prudect name : SC-203877;5-[3-Methoxy-4-(4-methoxy-benzyloxy)-benzyl]-pyrimidine-2,4-diamineGW2580 Synonyms: CAS NO: 870483-87-7Molecular Formula: C20H22N4O3Molecular Weight: 366.41368Purity: 98% minSolubility: In DMSOStorage: −20°C JTC801 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18517032

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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.

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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