361571

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
• Wzór empiryczny (zapis Hilla): C₂₂H₁₈Cl₂N₈
• Numer CAS: 252917-06-9
• Masa cząsteczkowa: 465.34
• UNSPSC Code: 12352200
• NACRES: NA.28
• MDL number: MFCD11846251
• Assay: ≥95% (HPLC)
• Form: liquid
• Quality level: 100
• Storage condition: OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

Właściwości

• Nazwa produktu: GSK-3 Inhibitor XVI, CHIR99021, InSolution, ≥95%, 25 mM
• Quality Level: 100
• assay: ≥95% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light
• shipped in: ambient
• storage temp.: −70°C
• SMILES string: 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)
• InChI key: AQGNHMOJWBZFQQ-UHFFFAOYSA-N

Opis

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). Exhibits little or no activity toward 46 other enzymes (IC₅₀ >8.8 µM against 20 kinases and K_i ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (K_d ~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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
GSK-3 α and β

Reversible: yes

Target IC₅₀: 10 and 6.7 nM against GSK-3&alpha

Packaging

Packaged under inert gas

Physical form

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

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

Disclaimer

Toxicity: Irritant (B)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 10 - Combustible liquids
• wgk: WGK 2
• flash_point_f: 188.6 °F - closed cup - (refers to pure substance)
• flash_point_c: 87 °C - closed cup - (refers to pure substance)