(Z)-4-Hydroxytamoxifen (also called 4-OH-TAM) was previously characterized as an Estrogen Receptor antagonist and now found to improve genome-editing specificity in CRISPR-mediated gene editing. It can activate intein-linked inactive Cas9, reducing off-target. Such system has ~25-fold higher specificity than wtCas9. (Z)-4-Hydroxytamoxifen is a Tamoxifen metabolite to be used as chemotherapeutic agent. It exhibits greater potency than Tamoxifen.
CAS Number: 68047-06-3
Molecular Weight: 387.51
Related CAS Number:
Chemical Name: (Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol
Appearance: Solid powder
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM; EtOH up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Powder: 4oC for 1 year, -20oC for 3years. DMSO: 4oC 3 month.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4oC for short term (days to weeks), or -20oC for long term (months).
Drug Formulation: This drug may be formulated in DMSO
HS Tariff Code: 2934.99.9001
How to use
(Z)-4-Hydroxytamoxifen was used at 1μM final concentration in CRISPR-mediated gene editing experiments.
(Z)-4-Hydroxytamoxifen was used at 10mg/Kg orally for the in vivo animal models.
- Jordan VC, et al. A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. (1977) J Endocrinol. 75(2):305-16.
- Desta Z, et al. Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. (2004) J Pharmacol Exp Ther. 310(3):1062-75.
- Davis KM, et al. Small molecule-triggered Cas9 protein with improved genome-editing specificity (2015) Nat Chem Biol. 11(5):316-8.
Products are for research use only. Not for human use.
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