A potent and selective inhibitor of GSK3 (IC50s = 1.5 and 0.9 for human recombinant GSK3α and GSK2β

LY2090314 – 1 mg

Brand:
Cayman
CAS:
603288-22-8
Storage:
-20
UN-No:
Non-Hazardous - /

LY2090314 is potent and selective inhibitor of glycogen synthase kinase 3 (GSK3) with IC50 values of 1.5 and 0.9 nM for human recombinant GSK3α and GSK3β, respectively.{39184} It has >10-fold selectivity for GSK3 over a panel of 40 kinases at a concentration of 20 μM. LY2090314 induces time-dependent stabilization of β-catenin total protein and activates Wnt signaling in vitro. It has potent antiproliferative activity in BRAF wild-type/NRAS mutant and BRAF mutant melanoma cell lines (IC50s = 6.0-11.8 nM) but has limited to no activity in non-melanoma cell lines with (IC50s = 430 to >20,000 nM). Knockdown of β-catenin in A375 and M14 melanoma cells induces LY2090314 resistance in vitro, indicating that LY2090314-induced cell death is dependent upon Wnt activation. In vivo, LY2090314 reduces tumor volume in a murine A375 melanoma xenograft model as a single agent and synergizes with decabarzine for a greater antitumor effect. Formulations containing LY2090314 are under clinical investigation for the treatment of advanced solid tumors.{39185}  

 

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Description

A potent and selective inhibitor of GSK3 (IC50s = 1.5 and 0.9 for human recombinant GSK3α and GSK2β, respectively); has >10-fold selectivity for GSK3 against a panel of 40 kinases at a concentration of 20 μM; induces time-dependent stabilization of β-catenin total protein and activates Wnt signaling in vitro; has potent antiproliferative activity in BRAF wild-type/NRAS mutant and BRAF mutant melanoma cell lines (IC50s = 6.0-11.8 nM) but has limited to no activity in non-melanoma cell lines (IC50s = 430 to >20,000 nM); knockdown of β-catenin in A375 and M14 melanoma cells induces LY2090314 resistance in vitro; reduces tumor volume in a murine A375 xenograft model as a single agent and synergizes with decabarzine for a greater antitumor effect,

Formal name: 3-[9-fluoro-1,2,3,4-tetrahydro-2-(1-piperidinylcarbonyl)pyrrolo[3,2,1-jk][1,4]benzodiazepin-7-yl]-4-imidazo[1,2-a]pyridin-3-yl-1H-pyrrole-2,5-dione

Synonyms: 

Molecular weight: 512.5

CAS: 603288-22-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|GSK3||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|GSK3 Signaling||Research Area|Cancer|Cell Signaling|Wnt Signaling||Research Area|Cell Biology|Cell Signaling|Wnt Signaling

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