Chemical Name: 4-[(1Z)-1-[4-[2-(Dimethylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]phenol
Biological Activity(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 �M for NavM and human Nav, respectively in HEK cells); this inhibition is independent of estrogen receptor modulation. Chemotherapeutic agent.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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Simple and efficient production of (Z)-4-hydroxytamoxifen, a potent estrogen receptor modulator.
Yu and Forman
Small molecule-triggered Cas9 protein with improved genome-editing specificity.
Davis et al.
A monohydroxylated metabolite of tamox. with potent antioestrogenic activity.
Jordan et al.
Comprehensive evaluation of tamox. sequential biotransformation by the human cytochrome P450 system in vitro: Prominent roles for CYP3A and CYP2D6.
Desta et al.
Citations for (Z)-4-Hydroxytamoxifen
The citations listed below are publications that use Tocris products. Selected citations for (Z)-4-Hydroxytamoxifen include:
5 Citations: Showing 1 - 5
The BAF and PRC2 Complex Subunits Dpf2 and Eed Antagonistically Converge on Tbx3 to Control ESC Differentiation.
Authors: Zhang Et al.
Cell Stem Cell 2019;24:138
Paracrine Crosstalk between Fibroblasts and ER+ Breast Cancer Cells Creates an IL1β-Enriched Niche that Promotes Tumor Growth.
Authors: Chatterjee Et al.
PTK6 regulates growth and survival of endocrine therapy-resistant ER+ breast cancer cells.
Authors: Ito Et al.
NPJ Breast Cancer 2017;3:45
MTA1 is a novel regulator of autophagy that induces TAX resistance in breast cancer cells.
Authors: Lee Et al.
Alcohol Regulates Genes that Are Associated with Response to Endocrine Therapy and Attenuates the Actions of tamox. in Breast Cancer Cells.
Authors: Candelaria Et al.
PLoS One 2015;10:e0145061
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