別名

DNA-PK Inhibitor II - CAS 154447-35-5 - Calbiochem,NU7026, DNA-Dependent Protein Kinase Inhibitor II, 2-(Morpholin-4-yl)-benzo[h]chromen-4-one, LY293646

一般描述

A cell-permeable benzochromenone compound that acts as a potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK with an IC50 of 0.23 μM. It is highly selective towards DNA-PK over PI3K-related kinases (IC50 = 13 μM for PI 3-K and >100 μM 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. 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 μM for PI 3-K and >100 μM 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.

生化/生理作用

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

重懸

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

其他說(shuō)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.