422000
Kenpaullone
A potent, cell-permeable, and reversible inhibitor of glycogen synthase kinase-3β (IC50 = 230 nM), Lck (IC50= 470 nM), and cyclin-dependent kinases (Cdks).
别名:
Kenpaullone, 9-Bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, NSC-664704
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关于此项目
经验公式（希尔记法）:
C16H11BrN2O
化学文摘社编号:
分子量:
327.18
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
Brc1cc2c([nH]c3c2CC(=O)Nc4c3cccc4)cc1
InChI
1S/C16H11BrN2O/c17-9-5-6-14-11(7-9)12-8-15(20)18-13-4-2-1-3-10(13)16(12)19-14/h1-7,19H,8H2,(H,18,20)
InChI key
QQUXFYAWXPMDOE-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow-brown
solubility
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
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General description
A potent cell-permeable and reversible inhibitor of glycogen synthase kinase-3β (IC50 = 230 nM), Lck (IC50 = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC50 = 400 nM), Cdk2/cyclin A (IC50 = 680 nM), Cdk2/cyclin E (IC50 = 7.5 µM), and Cdk5/p25 (IC50 = 850 nM). Also inhibits other kinases such as c-Src (IC50 = 15 µM), casein kinase II (IC50 = 20 µM), ERK1 (IC50 = 20 µM), and ERK2 (IC50 = 9 µM). Inhibition is competitive with respect to ATP binding.
A potent, cell-permeable, and reversible inhibitor of glycogen synthase kinase-3β (IC50 = 230 nM), Lck (IC50 = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC50 = 400 nM), Cdk2/cyclin A (IC50 = 680 nM), Cdk2/cyclin E (IC50 = 7.5 µM), and Cdk5/p25 (IC50 = 850 nM). Also inhibits other kinases such as c-Src (IC50 = 15 µM), casein kinase II (IC50 = 20 µM), ERK1 (IC50 = 20 µM), and ERK2 (IC50 = 9 µM). Inhibition is competitive with respect to ATP binding.
Biochem/physiol Actions
Cell permeable: yes
Product competes with ATP.
Reversible: yes
Target IC50: 230 nM, 470 nM, 400 nM, 680 nM, 7.5 µM, 850 nM, 15 µM, 20 µM, 20 µM, 9 µM against glycogen synthase kinase-3β, Lck IC50, Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, c-Src, casein kinase II, ERK1, and ERK2
Packaging
Packaged under inert gas
Other Notes
Bain, J., et al. 2003. Biochem. J. 371, 199.
Buolamwini, J.K. 2000. Curr. Pharm. Des.6, 379.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.
Zaharevitz, D.W., et al. 1999. Cancer Res. 59, 2566.
Buolamwini, J.K. 2000. Curr. Pharm. Des.6, 379.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.
Zaharevitz, D.W., et al. 1999. Cancer Res. 59, 2566.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
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