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Chir99021

(CAS No:252917-06-9)

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.

CAS No:252917-06-9

Molecular Weight(MW):501.8

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

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COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	252917-06-9
Molecular formula(MF)	C₂₂H₁₈Cl₂N₈^.HCl
Molecular Weight(MW):	501.8
Alias	6-[2-[4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-ylamino]ethylamino]pyridine-3-carbonitrile;6-{2-[4-(2,4-Dichloro-phenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino]-ethylamino}-nicotinonitrile;CHIR-99021;CT99021

Solubility

In vitro	DMSO	78 mg/mL warmed (167.61 mM)
	Water	<1 mg/mL
	Ethanol	<1 mg/mL
In vivo	4% DMSO+30% PEG 300+ddH2O	3.5mg/mL

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.

Targets

GSK-3β ^[1]	GSK-3α ^[1]
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	Incubation Time	Activity Description	PMID
human SW982 cell	Growth inhibition assay		Inhibition of human SW982 cell growth in a cell viability assay, IC50=214.16 nM.	SANGER
human GCT cell	Growth inhibition assay		Inhibition of human GCT cell growth in a cell viability assay, IC50=306.72 nM.	SANGER
human 769-P cell	Growth inhibition assay		Inhibition of human 769-P cell growth in a cell viability assay, IC50=584.99 nM.	SANGER
human LOXIMVI cell	Growth inhibition assay		Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=588.32 nM.	SANGER
human D-336MG cell	Growth inhibition assay		Inhibition of human D-336MG cell growth in a cell viability assay, IC50=846.2 nM.	SANGER
human S-117 cell	Growth inhibition assay		Inhibition of human S-117 cell growth in a cell viability assay, IC50=921.31 nM.	SANGER
human D-247MG cell	Growth inhibition assay		Inhibition of human D-247MG cell growth in a cell viability assay, IC50=948.52 nM.	SANGER
human TYK-nu cell	Growth inhibition assay		Inhibition of human TYK-nu cell growth in a cell viability assay, IC50=1.079 Î¼M.	SANGER
human A498 cell	Growth inhibition assay		Inhibition of human A498 cell growth in a cell viability assay, IC50=1.3 Î¼M.	SANGER
human HepG2 cells	Function assay	3 h	Inhibition of GSK3-beta in human HepG2 cells assessed as incorporation of [3H]glucose into glycogen after 3 hrs by liquid scintillation counting	22261023
human BCPAP cell	Growth inhibition assay		Inhibition of human BCPAP cell growth in a cell viability assay, IC50=1.67 Î¼M.	SANGER
human KYSE-180 cell	Growth inhibition assay		Inhibition of human KYSE-180 cell growth in a cell viability assay, IC50=1.73 Î¼M.	SANGER
human MIA-PaCa-2 cell	Growth inhibition assay		Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50=1.76 Î¼M.	SANGER
human HCC1395 cell	Growth inhibition assay		Inhibition of human HCC1395 cell growth in a cell viability assay, IC50=1.78 Î¼M.	SANGER
human RS4-11 cell	Growth inhibition assay		Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=1.95 Î¼M.	SANGER
human NCI-H2122 cell	Growth inhibition assay		Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=2.28 Î¼M.	SANGER
human SNU-423 cell	Growth inhibition assay		Inhibition of human SNU-423 cell growth in a cell viability assayï¼ IC50=2.5 Î¼M.	SANGER
human SK-LMS-1 cell	Growth inhibition assay		Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=2.64 Î¼M.	SANGER
human RPMI-7951 cell	Growth inhibition assay		Inhibition of human RPMI-7951 cell growth in a cell viability assayï¼ IC50=2.7 Î¼M.	SANGER
human COLO-829 cell	Growth inhibition assay		Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=2.7654 Î¼M.	SANGER
human SCC-9 cell	Growth inhibition assay		Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=2.95 Î¼M.	SANGER
human A704 cell	Growth inhibition assay		Inhibition of human A704 cell growth in a cell viability assay, IC50=3.0812 Î¼M.	SANGER
human HOP-62 cell	Growth inhibition assay		Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=3.36054 Î¼M.	SANGER
human HCC1569 cell	Growth inhibition assay		Inhibition of human HCC1569 cell growth in a cell viability assay, IC50=3.48305 Î¼M.	SANGER
human A172 cell	Growth inhibition assay		Inhibition of human A172 cell growth in a cell viability assay, IC50=3.75498 Î¼M.	SANGER
human MOLT-16 cell	Growth inhibition assay		Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=3.88556 Î¼M.	SANGER
human TE-15 cell	Growth inhibition assay		Inhibition of human TE-15 cell growth in a cell viability assay, IC50=3.95343 Î¼M.	SANGER
human OE19 cell	Growth inhibition assay		Inhibition of human OE19 cell growth in a cell viability assay, IC50=3.96451 Î¼M.	SANGER
human MHH-ES-1 cell	Growth inhibition assay		Inhibition of human MHH-ES-1 cell growth in a cell viability assay, IC50=4.04545 Î¼M.	SANGER
human NKM-1 cell	Growth inhibition assay		Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=4.13971 Î¼M.	SANGER
human RCC10RGB cell	Growth inhibition assay		Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=4.29479 Î¼M	SANGER
human BxPC-3 cell	Growth inhibition assay		Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=4.70391 Î¼M.	SANGER
human ALL-PO cell	Growth inhibition assay		Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=4.83858 Î¼M.	SANGER
human SK-OV-3 cell	Growth inhibition assay		Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=4.9934 Î¼M.	SANGER
human SW1710 cell	Growth inhibition assay		Inhibition of human SW1710 cell growth in a cell viability assay, IC50=5.42456 Î¼M.	SANGER

... Click to View More Cell Line Experimental Data

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].