BML-277 (Synonyms: BML-277, C 3742, Checkpoint Kinase 2 Inhibitor II) |
Catalog No.GC11648 |
Chk2 inhibitor,potent and highly selective
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Cas No.: 516480-79-8
Sample solution is provided at 25 µL, 10mM.
BML-277 is novel, potent and highly selective inhibitor of the chk2 with the IC50 value of 15±6.9nM [1].
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.
Average Rating: 5
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