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
- Molecular Weight:
- 501.8
- MDL Number:
- MFCD29079432
- MOL File:
- 1782235-14-6.mol
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) |
FDA UNII | LMF6N91874 |
CHIR 99021 trihydrochloride price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Tocris | 4953 | CHIR99021trihydrochloride ≥98%(HPLC) | 1782235-14-6 | 10 | $260 | 2021-12-16 | Buy |
Tocris | 4953 | CHIR99021trihydrochloride ≥98%(HPLC) | 1782235-14-6 | 50 | $1065 | 2021-12-16 | Buy |
Usbiological | 254961 | CHIR 99021 trihydrochloride | 1782235-14-6 | 10mg | $531 | 2021-12-16 | Buy |
TRC | C292153 | CHIR99021Trihydrochloride | 1782235-14-6 | 1mg | $65 | 2021-12-16 | Buy |
ApexBio Technology | B5779 | CHIR99021trihydrochloride | 1782235-14-6 | 5mg | $70 | 2021-12-16 | Buy |
CHIR 99021 trihydrochloride Chemical Properties,Uses,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
CHIR 99021 trihydrochloride Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |
EMMX Biotechnology LLC | 888-539-0666 | info@emmx.com | United States | 8449 | 60 |
Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9833 | 58 |
Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 18892239720 | psaitong@jm-bio.com | China | 12308 | 58 |