(Z)-4-Hydroxytamoxifen, Tocris Bioscience™

(Z)-4-Hydroxytamoxifen is an estrogen receptor antagonist (IC50 = 27 μM). (Z)-4-Hydroxytamoxifen is a Tamoxifen (Cat. No. 0999) metabolite; that exhibits greater potency than the parent compound. (Z)-4-Hydroxytamoxifen Also activates intein-linked inactive Cas9, reducing off-target CRISPR-mediated gene editing; system has ∽25-fold higher specificity than wtCas9. (Z)-4-Hydroxytamoxifen binds to voltage-gated sodium channels, near the intracellular gate and inhibits the sodium current by delaying channel recovery from the inactivated state (IC50 values are 297 nM and 2.1 μM for NavM and human Nav, respectively in HEK cells); this inhibition is independent of estrogen receptor modulation. Chemotherapeutic agent.