14-3-3 inhibitor BV2
Names
[ CAS No. ]:
302602-92-2
[ Name ]:
14-3-3 inhibitor BV2
[Synonym ]:
1,4-Benzenedicarboxylic acid, 2-[[(2,3-dihydro-1,5-dimethyl-3-oxo-2-phenyl-1H-pyrazol-4-yl)amino]carbonyl]-
2-[(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)carbamoyl]terephthalic acid
Biological Activity
[Description]:
A novel nonpeptidic inhibitor of 14-3-3 protein-protein interaction that promotes the apoptotic death of cells expressing either wt Bcr-Abl construct or T315I mutation; induces significant dose-dependent reduction of reproductive integrity of Ba/F3 cells expressing the wt and T315I-mutated Bcr-Abl with LD50 of 1.04 and 1.47 uM, respectively; promoted c-Abl release from 14-3-3σ, abolishes c-Abl expression in the cytoplasm, but has no influence on 14-3-3σ levels, induces apoptotic cell death in chronic myeloid leukemia sensitive or resistant to imatinib.
[References]
References 1. Mancini M, et al. J Pharmacol Exp Ther. 2011 Mar;336(3):596-604. 2. Mohammad DK, et al. Mol Cell Biol. 2013 Aug;33(16):3214-26. 3. Gómez-Suárez M, et al. Cell Death Differ. 2016 Jun;23(6):1060-72. 4. Valensin D, et al. Bioorg Med Chem Lett. 2016 Feb 1;26(3):894-898. View Related Products by Target 14-3-3 Protein
Chemical & Physical Properties
[ Density]:
1.5±0.1 g/cm3
[ Molecular Formula ]:
C20H17N3O6
[ Molecular Weight ]:
395.366
[ Exact Mass ]:
395.111725
[ LogP ]:
0.08
[ Index of Refraction ]:
1.714