CHIR-99021 (CT99021)

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Purity: >97%

Keywords

CHIR-99021 CT99021 252917-06-9

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Biological Activity

Description

CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.

Targets

GSK-3β [1] (Cell-free assay)	GSK-3α [1] (Cell-free assay)
6.7 nM	10 nM

In vitro

CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763 μM[1].

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
LOUCY	Growth Inhibition Assay	IC50=182.688 μM	SANGER
SN12C	Growth Inhibition Assay	IC50=182.829 μM	SANGER
A427	Growth Inhibition Assay	IC50=184.631 μM	SANGER

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Assay

Methods	Test Index	PMID
Western blot	Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin; CTNNB1; β-catenin;	30709379 23993102 24165128
Growth inhibition assay	Cell viability;	22039301
Immunofluorescence	SOX10/EdU; Oct3/4;	28174705 24779365

In vivo

Oral administration of CHIR-99021 at 30 mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150 mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels. Oral administration of CHIR-99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16 mg/kg and 48 mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge[1].

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