220486
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).
Synonym(s):
Chk2 Inhibitor II, 2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide
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About This Item
Empirical Formula (Hill Notation):
C20H14ClN3O2
CAS Number:
Molecular Weight:
363.80
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Pricing and availability is not currently available.
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Quality Level
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
1 of 4
This Item | 238811 | 220488 | 218860 |
|---|---|---|---|
| form solid | form solid | form solid | form solid |
| assay ≥95% (HPLC) | assay ≥95% (HPLC) | assay ≥95% (HPLC) | assay ≥99% (HPLC) |
| manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® |
| Quality Level 100 | Quality Level 100 | Quality Level 100 | Quality Level 100 |
| storage temp. 2-8°C | storage temp. 2-8°C | storage temp. −20°C | storage temp. 2-8°C |
| solubility DMSO: 5 mg/mL | solubility DMSO: 10 mg/mL, ethanol: 5 mg/mL | solubility DMSO: 5 mg/mL | solubility DMSO: 50 mg/mL |
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).
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
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Arienti, K. L., et al. 2005. J. Med. Chem.48, 1873.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
Certificates of Analysis (COA)
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