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361559

Sigma-Aldrich

GSK-3 Inhibitor XVI

GSK-3 Inhibitor XVI - CAS 252917-06-9, is a cell-permeable, potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC₅₀ = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively).

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Synonym(s):
GSK-3 Inhibitor XVI, 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile, CHIR99021
Empirical Formula (Hill Notation):
C22H18Cl2N8
CAS Number:
Molecular Weight:
465.34
MDL number:

Quality Level

Assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

light beige

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°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)

InChI key

AQGNHMOJWBZFQQ-UHFFFAOYSA-N

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361571361553361555
GSK-3 Inhibitor XVI GSK-3 Inhibitor XVI - CAS 252917-06-9, is a cell-permeable, potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC₅₀ = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively).

Sigma-Aldrich

361559

GSK-3 Inhibitor XVI

GSK-3β Inhibitor XI The GSK-3β Inhibitor XI, also referenced under CAS 626604-39-5, controls the biological activity of GSK-3β. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

361553

GSK-3β Inhibitor XI

GSK-3 Inhibitor XIII The GSK-3 Inhibitor XIII, also referenced under CAS 404828-08-6, controls the biological activity of GSK-3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

361555

GSK-3 Inhibitor XIII

form

solid

form

liquid

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

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

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

color

light beige

color

-

color

orange-red

color

white

solubility

DMSO: 5 mg/mL

solubility

-

solubility

DMSO: 5 mg/mL

solubility

DMSO: 5 mg/mL

General description

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). CHIR99021 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). CHIR99021 is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo.
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. Also available as a 25 mM solution in DMSO (Cat. No. 361571).

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

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.

Legal Information

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

Pictograms

Exclamation mark

Signal Word

Warning

Hazard Statements

Precautionary Statements

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

No data available

Flash Point(C)

No data available


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