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CHIR 99021 trihydrochloride

Product Name
CHIR 99021 trihydrochloride
CAS No.
1782235-14-6
Chemical Name
CHIR 99021 trihydrochloride
Synonyms
CHIR-99021 3HCl;CT-99021 trihydrochloride);CHIR 99021 trihydrochloride;Laduviglusib trihydrochloride;Laduviglusib (CHIR99021) trihydrochloride;CHIR 99021 trihydrochloride (252917-06-9 free base);CHIR-99021 trihydrochloride (CT99021 trihydrochloride;CT99021 TRIHYDROCHLORIDE;CHIR99021 TRIHYDROCHLORIDE;CHIR 99021 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;6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile trihydrochloride
CBNumber
CB63037186
Molecular Formula
C22H19Cl3N8
Formula Weight
501.8
MOL File
1782235-14-6.mol
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CHIR 99021 trihydrochloride Property

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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Tocris
Product number
4953
Product name
CHIR99021trihydrochloride
Purity
≥98%(HPLC)
Packaging
10
Price
$260
Updated
2021/12/16
Tocris
Product number
4953
Product name
CHIR99021trihydrochloride
Purity
≥98%(HPLC)
Packaging
50
Price
$1065
Updated
2021/12/16
Usbiological
Product number
254961
Product name
CHIR 99021 trihydrochloride
Packaging
10mg
Price
$531
Updated
2021/12/16
TRC
Product number
C292153
Product name
CHIR99021Trihydrochloride
Packaging
1mg
Price
$65
Updated
2021/12/16
ApexBio Technology
Product number
B5779
Product name
CHIR99021trihydrochloride
Packaging
5mg
Price
$70
Updated
2021/12/16
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CHIR 99021 trihydrochloride Chemical Properties,Usage,Production

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 trihydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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CHIR 99021 trihydrochloride Suppliers

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  • 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)
  • Laduviglusib trihydrochloride
  • Laduviglusib (CHIR99021) trihydrochloride
  • 1782235-14-6