361559
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).
別名:
GSK-3 Inhibitor XVI, 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile, CHIR99021
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この商品について
実験式（ヒル表記法）:
C22H18Cl2N8
CAS番号:
分子量:
465.34
UNSPSC Code:
12352200
NACRES:
NA.28
MDL number:
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
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
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
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 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
Preparation Note
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.
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: Harmful (C)
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
No data available
flash_point_c
No data available
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Deleterious substance
pdsc