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Merck

220491

Chk2 Inhibitor II

InSolution, ≥95%

Synonym(s):

InSolution 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
UNSPSC Code:
12352200
MDL number:
Assay:
≥95% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light
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Quality Level

assay

≥95% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

shipped in

ambient

storage temp.

−20°C

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

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. The solid form of this compound (Cat. No. 220486) is also available.

Packaging

Packaged under inert gas

Physical form

Supplied as a 25 mM (5 mg/550 µL) solution of Chk2 Inhibitor II (Cat. No. 220486) in DMSO.

Preparation Note

Following initial thaw, aliquot and freeze (-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

Disclaimer

Toxicity: Irritant (B)


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Storage Class

10 - Combustible liquids

wgk

WGK 2

flash_point_f

188.6 °F - closed cup - (refers to pure substance)

flash_point_c

87 °C - closed cup - (refers to pure substance)



Certificates of Analysis (COA)

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Ting-Yu Chen et al.
Cell death and differentiation, 28(6), 1865-1879 (2021-01-20)
The DNA-PK maintains cell survival when DNA damage occurs. In addition, aberrant activation of the DNA-PK induces centrosome amplification, suggesting additional roles for this kinase. Here, we showed that the DNA-PK-p53 cascade induced primary cilia formation (ciliogenesis), thus maintaining the