AdipoGen 4-Hydroxytamoxifen
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Chemical. CAS 68392-35-8. Formula C26H29NO2. MW 387.51. 4-Hydroxytamoxifen is an active metabolite of the chemotherapeutic drug tamoxifen, a selective estrogen receptor modulator SERM that acts as an agonist or antagonist in various tissues. 4-Hydroxytamoxifen acts as a tissue-selective agonist-antagonist of the estrogen receptors ERalpha and ERbeta. 4-Hydroxytamoxifen is an isoform-specific inhibitor of orphan estrogen-receptor-related ERR nuclear receptors beta and gamma. 4-Hydroxytamoxifen exhibits anticancer chemotherapeutic activity, inducing autophagy and vacuole formation as well as KRAS degradation in various cancer cell lines. In cardiac myocytes, 4-hydroxytamoxifen decreases Ca2 amplitude, slowing relaxation and decreasing contractility. 4-Hydroxytamoxifen has also shown to be a potent inhibitor of the mitochondrial permeability transition MPT.