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361571

Sigma-Aldrich

CHIR99021

≥95% (HPLC), liquid, GSK-3 inhibitor, Calbiochem

Sinônimo(s):

InSolution GSK-3 Inhibitor XVI, CHIR99021, 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile

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About This Item

Fórmula empírica (Notação de Hill):
C22H18Cl2N8
Número CAS:
252917-06-9
Peso molecular:
465.34
Número MDL:
MFCD11846251
Código UNSPSC:
12352200
NACRES:
NA.28

product name

GSK-3 Inhibitor XVI, CHIR99021, InSolution, ≥95%, 25 mM

Nível de qualidade

100

Ensaio

≥95% (HPLC)

forma

liquid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light

Condições de expedição

ambient

temperatura de armazenamento

−70°C

InChI

1S/C22H18Cl2N8/c1-13-10-29-21(31-13)17-12-30-22(32-20(17)16-4-3-15(23)8-18(16)24)27-7-6-26-19-5-2-14(9-25)11-28-19/h2-5,8,10-12H,6-7H2,1H3,(H,26,28)(H,29,31)(H,27,30,32)

chave InChI

AQGNHMOJWBZFQQ-UHFFFAOYSA-N

Descrição geral

A cell-permeable aminopyrimidine compound that acts as potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC50 = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively). Exhibits little or no activity toward 46 other enzymes (IC50 >8.8 µM against 20 kinases and Ki ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~4 µM). This compound is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo. The solid form of this compound (Cat. No. 361559) is also available.

Ações bioquímicas/fisiológicas

Cell permeable: yes
Primary Target
GSK-3 α and β
Reversible: yes
Target IC50: 10 and 6.7 nM against GSK-3&alpha

Embalagem

Packaged under inert gas

Advertência

Toxicity: Irritant (B)

forma física

A 25 mM (5 mg/430 µL) solution of GSK-3 Inhibitor XVI, CHIR99021 (Cat. No. 361559) in DMSO.

Outras notas

Mussmann, R., et al. 2007. J. Biol. Chem.282, 12030.
Ring, D.B., et al. 2003. Diabetes52, 588.
Bennett, C.N., et al. 2002. J. Biol. Chem.277, 30998.
Cline, G.W., et al. 2002.
Diabetes51, 2903.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Código de classe de armazenamento

10 - Combustible liquids

Classe de risco de água (WGK)

WGK 2

Ponto de fulgor (°F)

188.6 °F - closed cup - (refers to pure substance)

Ponto de fulgor (°C)

87 °C - closed cup - (refers to pure substance)

Certificados de análise (COA)

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