CHIR 99021 trihydrochloride
CHIR 99021 trihydrochloride Basic information
- Product Name:
- CHIR 99021 trihydrochloride
- Synonyms:
-
- CHIR 99021 trihydrochloride
- CHIR-99021 3HCl
- CT99021 TRIHYDROCHLORIDE;CHIR99021 TRIHYDROCHLORIDE;CHIR 99021 TRIHYDROCHLORIDE;CT-99021 TRIHYDROCHLORIDE
- 6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile trihydrochloride
- CHIR-99021 trihydrochloride (CT99021 trihydrochloride
- CT-99021 trihydrochloride)
- 6-((2-((4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile trihydrochloride
- CHIR 99021 trihydrochloride (252917-06-9 free base)
- CAS:
- 1782235-14-6
- MF:
- C22H19Cl3N8
- MW:
- 501.8
- Mol File:
- 1782235-14-6.mol
CHIR 99021 trihydrochloride Chemical Properties
- 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
CHIR 99021 trihydrochloride Usage And Synthesis
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.
target
| GSK-3β < span> 6.7 nM (IC 50 ) | GSK-3α 10 nM (IC 50 ) | cdc2 < span> 8800 nM (IC 50 ) |
storage
-20°C
CHIR 99021 trihydrochlorideSupplier
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