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.