Biochem/physiol Actions

BMS-189453 specifically has sufficient bioavailability in rats and monkeys. BMS-189453 only binds to α, β, and 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. Thus, it serves to treat rheumatoid arthritis.

BMS-189453 is a potent RARβ agonist that acts as an antagonist against RARα and RARγ. BMS-189453 induces RARβ reporter gene expression at sub nanomolar levels, and 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 activity, but 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.

Features and Benefits

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Packaging

5, 25 mg in glass bottle