CHIR-98014

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Cat No.

CEI-0087

Description

CHIR-98014 can inhibit GSK-3alpha and GSK-3beta with Ki of 0.65 nM and 0.58 nM.

CAS_No

252935-94-7

Molecular Weight

486.31

Purity

>99%

Storage

2 years at -20 centigrade

Targets

GSK-3alpha, GSK-3beta

Molecular Formula

C20H17Cl2N9O2

Chemical Name

N2-(2-(4-(2,4-dichlorophenyl)-5-(1H-imidazol-1-yl)pyrimidin-2-ylamino)ethyl)-5-nitropyridine-2,6-diamine

Solubility

DSMO 4 mg/mL Water

In vitro

CHIR-98014 can inhibit GSK-3alpha and GSK-3beta with Ki of 0.65 nM and 0.58 nM. CHIR-98014 is a ATP binding competitive inhibitor and shows 500-fold to 10,000-fold selectivity for GSK-3 versus 20 other protein kinases. CHIR 98014 also showed similar potency against the highly homologous and isoforms of GSK-3, it is noteworthy that they strongly discriminated between GSK-3 and its closest homologs cdc2 and erk2. CHIR-98014 can activate glycogen synthase at approximately 100 nmol/l in cultured CHO cells transfected with the insulin receptor.

In vivo

In primary hepatocytes isolated from Sprague-Dawley rats, and at 500 nmol/l in isolated type 1 skeletal muscle of both lean Zucker and ZDF rats. CHIR-98014 can enhance insulin-stimulated glucose transport in type 1 skeletal muscle from the insulin-resistant ZDF rats but not from insulin-sensitive lean Zucker rats. Single oral doses of CHIR-98014 (30-48 mg/kg) rapidly lowered blood glucose levels and improved glucose disposal after oral or intravenous glucose challenges in ZDF rats and db/db mice, without causing hypoglycemia or markedly elevating insulin.

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