CT99021 TRIHYDROCHLORIDE

CT99021 TRIHYDROCHLORIDE - Names and Identifiers

Name	CHIR-99021 (trihydrochloride)
Synonyms	CHIR-99021 3HCl CT99021 TRIHYDROCHLORIDE CT-99021 TRIHYDROCHLORIDE CHIR99021 TRIHYDROCHLORIDE CT-99021 trihydrochloride) CHIR 99021 trihydrochloride CHIR 99021 TRIHYDROCHLORIDE CHIR-99021 (trihydrochloride) CHIR 99021 trihydrochloride (252917-06-9 free base) CHIR-99021 trihydrochloride(CT99021 trihydrochloride 6-((2-((4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile trihydrochloride 6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile trihydrochloride
CAS	1782235-14-6

CT99021 TRIHYDROCHLORIDE - Physico-chemical Properties

Molecular Formula	C22H19Cl3N8
Molar Mass	501.8
Solubility	DMSO: ≥ 32 mg/mL
Storage Condition	-20℃
In vitro study	CHIR-99021 inhibits human GSK-3β with K i values of 9.8 nM. 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 (IC 50 =~5 nM) and GSK3α (IC 50 =~10 nM), with little effect on other kinases. 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 IC 50 of 4.9 μM.
In vivo study	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. 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.

CT99021 TRIHYDROCHLORIDE - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	1.74 ml	8.7 ml	17.4 ml
5 mM	0.348 ml	1.74 ml	3.48 ml
10 mM	0.174 ml	0.87 ml	1.74 ml
5 mM	0.035 ml	0.174 ml	0.348 ml

Last Update：2024-01-02 23:10:35

CT99021 TRIHYDROCHLORIDE - Reference Information

biological activity

CHIR-99021 trihydroxychloride (CT99021 trihydroxychloride) is a potent and selective GSK-3α/β inhibitor, the IC50 was 10 nM and 6.7 nM. CHIR-99021 trihydrochloride was more than 500-fold more selective for GSK-3 than CDC2,ERK2 and other protein kinases. CHIR-99021 trihydrochloride is also a potent activator of the Wnt/β-catenin signaling pathway. CHIR-99021 trihydrochloride enhances self-renewal of mouse and human embryonic stem cells. CHIR-99021 trihydrochloride can induce autophagy.

Last Update：2024-04-09 22:09:11