TMS is a potent and selective inhibitor of the EROD activity of P450 1B1 (CYP1B1) with IC50 of 6 nM.
TMS exhibits 50-fold selectivity for P450 1B1 over P450 1A1 (IC50=300 nM) and 500-fold selectivity for P450 1B1 over P450 1A2 (IC50=3 uM).
TMS blocks the conversion of estradiol to 4-OH-estradiol, inhibits tubulin polymerization and microtubule formation, causes cell cycle block at the G2-M phase, and induces apoptosis.
TMS significantly attenuates hypoxic PAH and hypoxic+SU5416 PAH in vivo (3mg/kg, i.p.).
