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361571

Sigma-Aldrich

CHIR99021

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

Synonim(y):

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

Wzór empiryczny (zapis Hilla):
C22H18Cl2N8
Numer CAS:
252917-06-9
Masa cząsteczkowa:
465.34
Numer MDL:
MFCD11846251
Kod UNSPSC:
12352200
NACRES:
NA.28

Nazwa produktu

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

Poziom jakości

100

Próba

≥95% (HPLC)

Formularz

liquid

producent / nazwa handlowa

Calbiochem®

warunki przechowywania

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

Warunki transportu

ambient

temp. przechowywania

−70°C

ciąg 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)

Klucz InChI

AQGNHMOJWBZFQQ-UHFFFAOYSA-N

Opis ogólny

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.

Działania biochem./fizjol.

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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Irritant (B)

Postać fizyczna

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

Inne uwagi

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.

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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Kod klasy składowania

10 - Combustible liquids

Klasa zagrożenia wodnego (WGK)

WGK 2

Temperatura zapłonu (°F)

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

Temperatura zapłonu (°C)

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

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