BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC 50 of 15 nM.
性状
Solid
IC50 & Target[1][2]
Chk2 15 nM (IC50)
体外研究(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 EC50 of 3?7.6 μM. The concentration of BML-277 required for radioprotection is consistent with the biochemical measurement of chk2 inhibition. Providing theKm of ATP for Chk2 is determined to be 99 μM and the Ki for 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 22.22 mg/mL (61.08 mM; Need ultrasonic)配制储备液