166977-43-1

BMS 453 is a synthetic retinoid and RARβ antagonist which also displays antagonist acitivity in RARα.

ChEBI: BMS-453 is a member of the class of dihydronaphthalenes that is 1,2-dihydronaphthalene which is substituted at positions 1, 1, 4, and 6 by methyl, methyl, phenyl, and 2-(p-carboxyphenyl)vinyl groups, respectively (the E isomer). It is a potent retinoic acid receptor gamma (RARbeta) agonist that acts as an antagonist against RARalpha and RARgamma. It has a role as a retinoic acid receptor beta agonist, a retinoic acid receptor gamma antagonist, a retinoic acid receptor alpha antagonist and a teratogenic agent. It is a member of dihydronaphthalenes, a member of benzoic acids and a stilbenoid.

BMS-189453 is a potent RARβ agonist th at acts as an antagonist against RARα and RARγ. BMS-189453 induces RARβ reporter gene expression at sub nanomolar levelsand is 30 fold more potent than all-trans retinoic acid for inducing TGFβ activity in normal breast cells. The compound BMS-189453 does not transactivate RARα or γ transcriptional activitybut binding to those family members induces a strong transrepression of phorbol ester-induced AP-1 activity (IC50 = 0.1 nM in HeLa and MCSF-7). BMS-189453 significantly increases the efficiency of cardiac differentiation of hESCs.''BMS-189453 specifically has sufficient bioavailability in rats and monkeys. BMS-189453 only binds to αβand γ retinoid receptors but its activation is unknown. BMS-189453 is found to inhibit the action of collagenase-3 (MMP-13) which catalyses cartilage matrix degradation. Thusit serves to tre at rheumatoid