Basic information Safety Supplier Related

CHIR 99021 trihydrochloride

Basic information Safety Supplier Related

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
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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)
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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

EMMX Biotechnology LLC
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888-539-0666
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info@emmx.com
Amadis Chemical Company Limited
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571-89925085
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sales@amadischem.com
Beijing Jin Ming Biotechnology Co., Ltd.
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010-60605840 18892239720
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psaitong@jm-bio.com
Dezhou LonWel Pharmaceutical Technology Co., Ltd.
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13761310616
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Musechem
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+1-800-259-7612
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