DNA-PK Inhibitor II-CAS 154447-35-5-Calbiochem

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一般描述

A cell-permeable, potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK (IC₅₀= 230 nM). Reported to be highly selective for DNA-PK compared to PI3 K-related kinases (IC₅₀= 13 ?M for PI 3-K and >100 ?M for ATM and ATR). Exhibits no inhibitory effect on PARP-1. Shown to inhibit DNA-PK-mediated, but not PARP-1-mediated, cellular DNA double strand break (DSB) repair and potentially lethal damage recovery (PLDR) following ionizing radiation (IR). Also shown to sensitize both proliferating and quiescent cells to IR.
A cell-permeable benzochromenone compound that acts as a potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK with an IC₅₀of 0.23 ?M. It is highly selective towards DNA-PK over PI3K-related kinases (IC₅₀= 13 ?M for PI 3-K and >100 ?M for ATM and ATR) and has no effect on PARP-1. Inhibits DNA-PK-mediated, but not PARP-1-mediated, cellular DNA DSB (double strand break) repair and PLDR (potentially lethal damage recovery) following IR (ionizing radiation). Shown to sensitize both proliferating and quiescent cells to IR.

包装

5 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Target IC₅₀: 0.23 ?M against DNA-PK
Primary Target
DNA-PK
Product competes with ATP.
Reversible: yes

警告

Toxicity: Carcinogenic / Teratogenic (D)

重悬

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Willmore, E., et al. 2004.Blood,103,4659.
Hollick, J.J., et al. 2003.Bioorg. Med. Chem. Lett.13,3083.
Veuger, S.J., et al. 2003.Cancer Res.63,6008.
Vlahos, C.J., et al. 1994.J. Biol. Chem.269,5241.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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