Product Description
A selective inhibitor of aromatase (estrogen synthetase) would be a useful pharmacological
tool with potential therapeutic application. We have found that 6 alpha-bromoandrostenedione
(6 alpha-BrA) is a competitive inhibitor of human placental aromatase with respect to
androstenedione, with an apparent Ki of 3.4 nM, while 6 beta-BrA is a mechanism-based
irreversible inhibitor with an apparent Ki of 0.8 microM and a kinact of 0.025 min-1.
Aromatase activity was measured by tritium release into water from the 1 beta position of
[1(-3)H,4(-14)C]androstenedione in reaction mixtures containing NADPH and the aromatase.