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Key Documents

361571

Sigma-Aldrich

CHIR99021

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

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C22H18Cl2N8
Numero CAS:
Peso molecolare:
465.34
Numero MDL:
Codice UNSPSC:
12352200
NACRES:
NA.28

product name

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

Livello qualitativo

Saggio

≥95% (HPLC)

Forma fisica

liquid

Produttore/marchio commerciale

Calbiochem®

Condizioni di stoccaggio

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

Condizioni di spedizione

ambient

Temperatura di conservazione

−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)
AQGNHMOJWBZFQQ-UHFFFAOYSA-N

Descrizione generale

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.

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Irritant (B)

Stato fisico

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

Altre note

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.

Note legali

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

Codice della classe di stoccaggio

10 - Combustible liquids

Classe di pericolosità dell'acqua (WGK)

WGK 2

Punto d’infiammabilità (°F)

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

Punto d’infiammabilità (°C)

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


Certificati d'analisi (COA)

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