516480-79-8BML-277

产品属性：

Cas No.516480-79-8

别名

化学名 2-[4-(4-chlorophenoxy)phenyl]-3H-benzimidazole-5-carboxamide

分子式 C20H14ClN3O2

分子量 363.8

溶解度 ≥ 18.2mg/mL in DMSO

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
BML-277 has shown the ATP-competitive inhibition of chk2 with the Ki value of 37nM. BML-277 has also been exhibited to be a chk2 inhibitor with the IC50 value of 15±6.9nM and efficiently rescue T-cell populations from the apoptosis of radiation-induced in a concentration-dependent fashion with the EC50 of 3~7.6μM. The Km of ATP for chk2 is 99μM and assuming that intracellular ATP concentration is 10mM. Apart from these, BML-277 has shown the inhibition through docking into a homology model of chk2 ATP binging site [1].

References:

[1]Arienti KL1, Brunmark A, Axe FU, McClure K, Lee A, Blevitt J, Neff DK, Huang L, Crawford S, Pandit CR, Karlsson L, Breitenbucher JG. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.