CHIR 99021 trihydrochloride

CAS NO.：1782235-14-6
Empirical Formula: C22H19Cl3N8
Molecular Weight: 501.8
MDL number: MFCD29079432
Update Date: 2026-05-11 15:21:01

What is CHIR 99021 trihydrochloride?

Biological Activity

CHIR-99021 trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC50 of 10 nM and 6.7 nM. It is more than 500-fold selective for GSK-3 over CDC2, ERK2 and other protein kinases. Also CHIR-99021 trihydrochloride is a potent activator of Wnt/β-catenin signaling pathway. It enhances self-renewal in mouse and human embryonic stem cells.

in vitro

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 . it (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.

in vivo

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.

Storage

-20°C

Properties of CHIR 99021 trihydrochloride

storage temp.	Store at -20°C
solubility	DMSO:30.37(Max Conc. mg/mL);52.84(Max Conc. mM) Water:16.69(Max Conc. mg/mL);29.04(Max Conc. mM)
form	Solid
color	White to light yellow