CHIR-99021 (CT99021)

  Cat. No.:  DC1023   Featured
CHIR-99021 (CT99021)
Chemical Structure
252917-06-9
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Field of application
CHIR-99021 is a glycogen synthase kinase 3 beta inhibitor that has antiproliferative activity in vitro and in vivo.
Cas No.: 252917-06-9
Chemical Name: 6-((2-((4-(2,4-dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile
Synonyms: CHIR-911; CHIR911; CHIR 911; CT-99021; CT99021; CT 99021; CHIR-73911; CHIR73911; CHIR 73911; GSK 3 inhibitor XVI; GSK 3IXV; CHIR99021; CHIR 99021;
SMILES: CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N
Formula: C22H18Cl2N8
M.Wt: 465.34
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: CHIR-99021 is a GSK-3α/β inhibitor with an IC50 of 10 and 6.7 nM,showing 500-fold selectivity over its closest homologs CDC2 and ERK2, as well as other protein kinases.
In Vivo: In ZDF rats, a single oral dose of CHIR 99021 (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration[1]. CHIR99021 (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). CHIR99021 treatment significantly blocks crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. CHIR99021 treatment increases Lgr5+ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h[4].
In Vitro: CHIR 99021inhibits human GSK-3β with Ki values of 9.8 nM[1]. CHIR 99021 is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that CHIR 99021 specifically inhibits GSK3β (IC50=~5 nM) and GSK3α (IC50=~10 nM), with little effect on other kinases[2]. In the presence of CHIR-99021 the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM CHIR-99021 with an IC50 of 4.9 μM[3].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC1063 TWS119 TWS119 is a GSK-3β inhibitor with IC50 of 30 nM.
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DC4227 SB216763 SB 216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).
DC9726 CP21 (CP21R7) CP21R7 is a potent and selective GSK-3β inhibitor.
DC1023 CHIR-99021 (CT99021) CHIR-99021 is a glycogen synthase kinase 3 beta inhibitor that has antiproliferative activity in vitro and in vivo.
DC9703 CHIR-99021 HCl CHIR-99021 HCl is a glycogen synthase kinase 3 beta inhibitor that has antiproliferative activity in vitro and in vivo.
DC7384 CHIR-98014 CHIR-98014 is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.
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