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220486

Sigma-Aldrich

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.

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

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This Item
238811220488218860
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
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


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