361566
GSK-3 Inhibitor IV, SB-216763
別名:
GSK-3 Inhibitor IV, SB-216763, SB-216763
ログインで組織・契約価格をご覧ください。
サイズを選択してください
表示を変更する
この商品について
実験式（ヒル表記法）:
C19H12Cl2N2O2
CAS番号:
分子量:
371.22
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze
assay
≥98% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
orange
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
Clc1c(ccc(c1)Cl)C2=C(C(=O)NC2=O)c3c4c([n](c3)C)cccc4
InChI
1S/C19H12Cl2N2O2/c1-23-9-13(11-4-2-3-5-15(11)23)17-16(18(24)22-19(17)25)12-7-6-10(20)8-14(12)21/h2-9H,1H3,(H,22,24,25)
InChI key
JCSGFHVFHSKIJH-UHFFFAOYSA-N
General description
A cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (Ki = 9.1 nM for GSK-3α). At 10 µM concentration, does not significantly inhibit a panel of 24 other protein kinases tested. Reported to stimulate glycogen synthesis in Chang human liver cells (EC50 = 3.6 µM) and induce transcription of β-catenin-LEF/TCF (lymphoid enhancer factor/T cell factor) regulated reporter gene in HEK293 human embryonic kidney cell lines. Offers protection against polyglutamine-induced death in SK-N-SH and COS-7 cells and attenuates hypoxia-induced apoptosis in VSMC and COS-7 cells. Shown to reduce phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase) expression in hepatoma cells. Promotes the survival of CLL lymphocytes via Wnt/β-catenin-mediated transcription activation. Exhibits delayed cardioprotection in vivo in a rat model via a KATP (ATP-sensitive potassium channels) and MPTP (mitochondrial permeability transition pore)-dependent mechanism at reperfusion.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Gross, E., et al. 2008. Am. J. Phy. Heart Circ Physiol.294, H1497.
Bain, J., et al. 2007. Biochem. J.408, 297.
Lu, D., et al. 2004. PNAS.101, 3118.
Carmichael, J., et al. 2002. J. Biol. Chem.277, 33791.
Culbert, A.A., et al. 2001. FEBS Lett.507, 288.
Lochhead, P.A., et al. 2001. Diabetes50, 937.
Cross, D.A., et al. 2001. J. Neurochem.77, 94.
Coghlan, M.P., et al. 2000. Chem. Biol.7, 793.
Bain, J., et al. 2007. Biochem. J.408, 297.
Lu, D., et al. 2004. PNAS.101, 3118.
Carmichael, J., et al. 2002. J. Biol. Chem.277, 33791.
Culbert, A.A., et al. 2001. FEBS Lett.507, 288.
Lochhead, P.A., et al. 2001. Diabetes50, 937.
Cross, D.A., et al. 2001. J. Neurochem.77, 94.
Coghlan, M.P., et al. 2000. Chem. Biol.7, 793.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable