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all-trans-4-hydroxy Retinoic acid is a metabolite of all-trans retinoic acid formed by the cytochrome P450 (CYP) isoforms CYP26A1, B1, and C1. It binds to retinoic acid receptors (RARs) with a lower affinity than other all-trans retinoic acid metabolites (IC50s = 606, 298, and 892 nM for RARα, RARβ, and RARγ, respectively, in a radioligand binding assay). It also transactivates RARs with a lower efficacy than other metabolites (EC50s = 791, 64, and 94 nM for RARα, RARβ, and RARγ, respectively) but induces transcription of a reporter plasmid equipotently. all-trans-4-hydroxy Retinoic acid inhibits cell growth, halts the cell cycle in the G1 phase, and induces differentiation of NB4 acute promyelocytic leukemia cells (EC50 = 79.8 nM). |