Exemestane is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
Effect of exemestane on phosphatidylserine exposure. A. Original histogram of annexin-V-binding of erythrocytes following exposure for 48 hours to Ringer solution without (grey area) and with (black line) presence of 40 µg/ml exemestane. B. Arithmetic means ± SEM (n = 24) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) exemestane (10-40 µg/ml). For comparison, the effect of the solvent DMSO is shown (grey bar). **(p<0.01),***(p<0.001) indicates significant difference from the absence of exemestane (ANOVA).
Formestane is a second generation selective aromatase inhibitor with an IC50 of 80 nM.
Aminoglutethimide is an aromatase inhibitor with IC50 of 10 μM.
Alpha-Naphthoflavone, a synthetic flavonoid, is a potent inhibitor of aromatase with an I50 value of 0.5 μM.
Obacunone, a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2.