Product Description
BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 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 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[1].
Information
CAS No516480-79-8
FormulaC20H14ClN3O2
Clinical Informationclinicalinformation
PathwayCell Cycle/DNA Damage
TargetCheckpoint Kinase (Chk)
Specifications
Purity / Grade>98%
SolubilityDMSO : 50 mg/mL (137.44 mM; Need ultrasonic)
Smilessmiles
Misc Information
Storage InstructionStore at -20°C: ship with blue ice.
Alternative NamesChk2 Inhibitor II
Observed Molecular Weight363.8
NotesBML-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.
ProtocolFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.