Drug intelligence / Profile preview

BMS961

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Topical
01

Overview

BMS961 is a potent and selective agonist of the retinoic acid receptor gamma (RARγ), part of the nuclear receptor superfamily that regulates transcription, especially involved in growth arrest and differentiation of keratinocytes and other cells. BMS961 shows high selectivity for RARγ over other RAR subtypes, with IC50 (inhibitory concentration) values of 30 nM at RARγ and ~1000 nM at RARβ, and essentially no activity at RARα[1][3][6]. Its mechanism has been used to study retinoid biology, developmental biology (notably in limb outgrowth and chondrogenesis), and the regulation of specific genes related to these processes[4]. It has a molecular formula of C23H26FNO4 and CAS number 185629-22-5. BMS961 is for research use only and not for human or veterinary therapeutic applications[3].

Other names
BMS961BMS-961BMS 961BMS270394BMS-270394BMS 270394
02

Targets

RARB (Retinoic acid receptor beta)RARG (Retinoic acid receptor gamma)

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