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Merck

220486

Chk2 Inhibitor II

≥95% (HPLC), Chk2 inhibitor, solid

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:
516480-79-8
Molecular Weight:
363.80
MDL number:
MFCD08276917
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Product Name

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

100

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

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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Yu-Ying Chao et al.
Journal of cellular physiology (2022-10-18)
Pancreatic ductal adenocarcinoma (PDAC) is one of the most lethal cancers because of its late diagnosis and chemoresistance. Primary cilia, the cellular antennae, are observed in most human cells to maintain development and differentiation. Primary cilia are gradually lost during

Global Trade Item Number

SKUGTIN
220486-1MGCN04055977201147

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