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Merck

361571

Sigma-Aldrich

CHIR99021

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

Sinónimos:

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 (notación de Hill):
C22H18Cl2N8
CAS Number:
Peso molecular:
465.34
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.28

Product Name

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

Nivel de calidad

Ensayo

≥95% (HPLC)

Formulario

liquid

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

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

Condiciones de envío

ambient

temp. de almacenamiento

−70°C

cadena SMILES

Clc1c(ccc(c1)Cl)c2nc(ncc2c4[nH]cc(n4)C)NCCNc3ncc(cc3)C#N

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)

Clave InChI

AQGNHMOJWBZFQQ-UHFFFAOYSA-N

Descripción general

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.

Acciones bioquímicas o fisiológicas

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

Envase

Packaged under inert gas

Forma física

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

Otras 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.

Información legal

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

Cláusula de descargo de responsabilidad

Toxicity: Irritant (B)

Código de clase de almacenamiento

10 - Combustible liquids

Clase de riesgo para el agua (WGK)

WGK 2

Punto de inflamabilidad (°F)

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

Punto de inflamabilidad (°C)

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


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