A cell-permeable, reversible inhibitor of dynamin 1, dynamin 2, and mitochondrial dynamin, Drp1 GTPase activity (IC₅₀ = 15 μM); inhibits clathrin-dependent vesicle formation and endocytosis; can also augment the release of neurotransmitters and secreted cytokines.

A cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC₅₀ = 112 and 165 nM, respectively); has no detectable binding activity to either ERα or ERβ.

An non-nucleoside reverse transcriptase inhibitor that prevents RNA plus-strand initiation (IC₅₀ = 17 nM); also inhibits the late stages of HIV-1 replication by interfering with HIV-1 Gag-Pol polyprotein processing.

A natural metabolite formed by CYP450-mediated hydroxylation followed by catechol-O-methyltransferase (COMT) methylation of estradiol; has anticancer agent activity as an angiogenesis inhibitor via the HIF-1α pathway; levels are significantly lower in women with severe pre-eclampsia.