Estradiol 3-methyl ether (EDME) is a potent antagonist of the TRPML1 ion channel and a microtubule depolymerizer. It exhibits remarkable selectivity, with IC50 values of 0.22 μM against TRPML1 and 3.8 μM against TRPML2, while showing no activity towards TRPML3. EDME disrupts cytoplasmic microtubule networks in mammalian cells with an EC50 of 9 μM. This compound operates independently of estrogen receptors to block autophagy, inhibit TFEB nuclear translocation, and reduce migration and invasion in triple-negative breast cancer cells, making it highly relevant for research in cancer biology.
Estradiol 3-methyl ether (EDME) is a potent antagonist of the TRPML1 ion channel and a microtubule depolymerizer. It exhibits remarkable selectivity, with IC50 values of 0.22 μM against TRPML1 and 3.8 μM against TRPML2, while showing no activity towards TRPML3. EDME disrupts cytoplasmic microtubule networks in mammalian cells with an EC50 of 9 μM. This compound operates independently of estrogen receptors to block autophagy, inhibit TFEB nuclear translocation, and reduce migration and invasion in triple-negative breast cancer cells, making it highly relevant for research in cancer biology.
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