BMS 195614

Uses

BMS 195614, is a selective neutral RARα inhibitor and exhibits no significant effect on NCoR binding. It decreases agonist-induced coactivator recruitment and SMRT binding to RAR. RARs, or Retinoic Acid Receptors, are nuclear hormone receptors that form heterodimers with RXRs (Retinoid X Receptors).

Definition

ChEBI: BMS 195614 is a carboxamide resulting from the formal condensation of the carboxy group of 5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthalene-2-carboxylic acid with the amino group of p-aminobenzoic acid. It is a neutral retinoic acid receptor (RAR) alpha-selective antagonist (Ki = 2.5 nM). It displays no significant effect on nuclear receptor corepressor (NCoR) binding; moderately decreases SMRT binding to RAR. It antagonizes agonist-induced coactivator (CoA) recruitment. It has a role as a retinoic acid receptor alpha antagonist. It is a member of quinolines, a member of benzoic acids and a secondary carboxamide.