BML-277

"目录号: HY-13946

Cell Cycle/DNA Damage-

BML-277 是一种选择性的检测点激酶 2 (Chk2) 抑制剂，IC50为 15 nM。

Checkpoint Kinase (Chk)

相关产品

LY2606368-CCT241533 hydrochloride-AZD-7762-SCH900776-LY2603618-CCT245737-CHIR-124-PF 477736-CCT244747-

生物活性

Description

BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with anIC50of 15 nM.

IC50& Target

IC50: 15 nM (Chk2)[1]

In Vitro

BML-277 is an ATP-competitive inhibitor of Chk2 that dose dependently protects human CD4+and CD8+T-cells from apoptosis due to ionizing radiation. BML-277 efficiently rescues both T-cell populations from radiation-induced apoptosis in a dose-dependent manner with an observed EC50of 3?7.6 μM. The concentration of BML-277 required for radioprotection is consistent with the biochemical measurement of chk2 inhibition. Providing theKmof ATP for Chk2 is determined to be 99 μM and the Kifor BML-277 is 37 nM, and assuming that the intracellular ATP concentration is 10 mM, a 5 μM concentration of BML-277 would be expected to produce 42% inhibition of intracellular chk2[1].

References

[1].Arienti KL, et al. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.