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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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QC Documents
 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 Concentration Incubation Time Formulation 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 μM. SANGER
human A498 cell Growth inhibition assay Inhibition of human A498 cell growth in a cell viability assay, IC50=1.3 μM. 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 μM. SANGER
human KYSE-180 cell Growth inhibition assay Inhibition of human KYSE-180 cell growth in a cell viability assay, IC50=1.73 μM. 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 μM. SANGER
human HCC1395 cell Growth inhibition assay Inhibition of human HCC1395 cell growth in a cell viability assay, IC50=1.78 μM. SANGER
human RS4-11 cell Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=1.95 μM. SANGER
human NCI-H2122 cell Growth inhibition assay Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=2.28 μM. SANGER
human SNU-423 cell Growth inhibition assay Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=2.5 μM. 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 μM. SANGER
human RPMI-7951 cell Growth inhibition assay Inhibition of human RPMI-7951 cell growth in a cell viability assay, IC50=2.7 μM. SANGER
human COLO-829 cell Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=2.7654 μM. SANGER
human SCC-9 cell Growth inhibition assay Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=2.95 μM. SANGER
human A704 cell Growth inhibition assay Inhibition of human A704 cell growth in a cell viability assay, IC50=3.0812 μM. SANGER
human HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=3.36054 μM. SANGER
human HCC1569 cell Growth inhibition assay Inhibition of human HCC1569 cell growth in a cell viability assay, IC50=3.48305 μM. SANGER
human A172 cell Growth inhibition assay Inhibition of human A172 cell growth in a cell viability assay, IC50=3.75498 μM. SANGER
human MOLT-16 cell Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=3.88556 μM. SANGER
human TE-15 cell Growth inhibition assay Inhibition of human TE-15 cell growth in a cell viability assay, IC50=3.95343 μM. SANGER
human OE19 cell Growth inhibition assay Inhibition of human OE19 cell growth in a cell viability assay, IC50=3.96451 μM. 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 μM. SANGER
human NKM-1 cell Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=4.13971 μM. SANGER
human RCC10RGB cell Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=4.29479 μM SANGER
human BxPC-3 cell Growth inhibition assay Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=4.70391 μM. SANGER
human ALL-PO cell Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=4.83858 μM. 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 μM. SANGER
human SW1710 cell Growth inhibition assay Inhibition of human SW1710 cell growth in a cell viability assay, IC50=5.42456 μM. 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].