Nuclear retinoic acid receptors (RARs) are transcriptional regulators with roles in cell proliferation and differentiation. BMS 453 is a synthetic retinoid that acts as an agonist of RARβ and an antagonist of RARα and RARγ. It has been shown to inhibit the proliferation of normal breast cells via the induction of TGF-β activity, causing G1 arrest. BMS 453 binding to RARα and RARγ can induce a transrepression of phorbol ester-induced AP-1 activity (IC50s = ~0.1 nM in HeLa and MCSF-7 cells), which also correlates with reduced cell proliferation. BM 453 has been used to trigger the differentiation of mouse embryonic stem cells (mES) in a study of RARβ-induced mES cell adipogenesis.
