Estradiol 3-methyl ether

Estradiol 3-methyl ether (EDME) is a highly selective TRPML1 ion channel antagonist and microtubule (microtubule) depolymerizing agent, with IC₅₀ values of 0.22 μM and 3.8 μM against TRPML1 and TRPML2, respectively; it shows no activity against TRPML3. Estradiol 3-methyl ether induces the disruption of cytoplasmic microtubule networks in mammalian cells, with an EC₅₀ of 9 μM. Independent of estrogen receptors, Estradiol 3-methyl ether blocks autophagy (autophagy), TFEB nuclear translocation, and inhibits the migration and invasion of triple-negative breast cancer cells by suppressing TRPML1. Estradiol 3-methyl ether is applicable for relevant research on triple-negative breast cancer^[1][2]. In Vitro:Estradiol 3-methyl ether (1 μM; 3 h) inhibits TFEB nuclear translocation and blocks the induction of autophagy^[1].
Estradiol 3-methyl ether (0.1-10 μM) significantly inhibits the invasive ability of MDA-MB-231 WT cells in a dose-dependent manner^[1].
Estradiol 3-methyl ether (9-100 μM; 1 h) induces microtubule breakage in Chinese hamster V79 cells, with an EC₅₀ of 9 μM after 1 h of incubation, and completely abolishes the normal microtubule network at a concentration of 100 μM^[2].
Estradiol 3-methyl ether (20-50 μM; 2-4 days) inhibits the growth of Chinese hamster V79 cells, and treatment with 20 μM for 2 days causes 92% growth inhibition^[2].