220486
Chk2 Inhibitor II
≥95% (HPLC), Chk2 inhibitor, solid
别名:
Chk2 Inhibitor II, 2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide
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关于此项目
经验公式（希尔记法）:
C20H14ClN3O2
化学文摘社编号:
分子量:
363.80
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
Chk2 Inhibitor II, Chk2 Inhibitor II, BML-277, CAS 516480-79-8 is a cell-permeable, potent, reversible, ATP-competitive inhibitor of Chk2 (IC50 = 15 nM).
SMILES string
Clc1ccc(cc1)Oc2ccc(cc2)c3[nH]c4c(n3)cc(cc4)C(=O)N
InChI
1S/C20H14ClN3O2/c21-14-4-8-16(9-5-14)26-15-6-1-12(2-7-15)20-23-17-10-3-13(19(22)25)11-18(17)24-20/h1-11H,(H2,22,25)(H,23,24)
InChI key
UXGJAOIJSROTTN-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
potency
15 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
pale yellow
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Ki = 37 nM inhibiting Chk2.EC50 = 3 µM and 7.6 µM in rescuing both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis
Primary Target
Chk2
Chk2
Product competes with ATP.
Reversible: yes
Target Ki: 37 nM inhibiting Chk2
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable and reversible benzimidazolo compound that acts as a potent and ATP-competitive inhibitor of Chk2 with an IC50 of 15 nM and a Ki of 37 nM. Displays ~ 1,000-fold greater selectivity over Cdk1/B and CK1 (IC50 = 12 M and 17 M, respectively) and only weakly affects the activities of a panel of 31 kinases (<25% inhibition at 10 M), including Chk1. Shown to rescue both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis with an EC50 of 3 M and 7.6 M, respectively. Also available as a 25 mM solution in DMSO (Cat. No. 220491).
Other Notes
Arienti, K. L., et al. 2005. J. Med. Chem.48, 1873.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
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