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Beschreibung

A cell-permeable salicylic acid compound that acts as a highly potent, active-site directed and substrate competitive AKR1C1 inhibitor (Ki = 4 nM) with moderate to excellent selectivity over AKR1C2, AKR1C3 and AKR1C4 (Ki = 0.087, 4.2 and 18.2 µ,M, respectively). Shown to inhibit the metabolism of progesterone by AKR1C1 (IC50 = 460 nM in AKR1C1 overexpressing BAECs).