2-hydroxy Estradiol (2-HE2) is a cytochrome P450 metabolite of estradiol with low affinity for estrogen receptors. 2-HE is rapidly metabolized by catechol-O-methyltransferase (COMT) to form 2-methoxy estradiol (2-ME2) with a half-life of approximately ten minutes in rat. 2-ME2 has achieved considerable attention as an anti-cancer agent acting as an angiogenesis inhibitor via the HIF-1a pathway. Due to the rapid metabolism of 2-HE2, the effects attributed to 2-HE2, may actually be those of 2-ME2.
