An aminopyrimidine derivative that inhibits GSK3α and GSK3β (IC50s = 10 and 6.7 nM

CHIR99021 – 5 mg

Brand:
Cayman
CAS:
252917-06-9
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that plays a key inhibitory role in both the insulin and Wnt signaling pathways.{14419,14420} CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively.{19045} When tested against twenty different protein kinases, this inhibitor shows greater than 500-fold selectivity for GSK3.{19045} CHIR99021 activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle.{19045} A single oral dose (30 mg/kg) of CHIR99021 enhances in vivo glucose metabolism in a rodent model of type 2 diabetes.{19045} CHIR99021 has also been shown to induce the reprogramming of murine and human somatic cells into stem cells.{19047,16878}  

 

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Description

An aminopyrimidine derivative that inhibits GSK3α and GSK3β (IC50s = 10 and 6.7 nM, respectively); activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle; has been shown to promote self-renewal of embryonic stem cells

Formal name: 6-[[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile

Synonyms:  CT 99021

Molecular weight: 465.3

CAS: 252917-06-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|GSK3||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Stem Cell Research|Reprogramming||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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