302602-92-2

302602-92-2 structure

Name: 14-3-3 inhibitor BV2
Chemical Name: 2-[(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)carbamoyl]terephthalic acid
CAS Number: 302602-92-2
Molecular Formula: C₂₀H₁₇N₃O₆
Molecular Weight: 395.366
Create Date: 2020-01-11 17:06:00
Modify Date: 2024-04-02 18:59:34
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.

Name	2-[(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)carbamoyl]terephthalic acid
Synonyms	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

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