(Z)-4-Hydroxytamoxifen, CRISPR Editing Enhancer


Catalog No. size PriceQuantity
M60324-2S 2 mg solid $89
M60324-10S 10mg solid $356

Description

Product Information
Molecular Weight: 387.51
Formula: C26H29NO2
Purity: ≥98%
CAS#: 68047-06-3
Solubility: DMSO up to 100 mM; EtOH up to 50 mM
Chemical Name: (Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

(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.

How to Use:

In vitro: 
(Z)-4-Hydroxytamoxifen was used at 1μM final concentration in CRISPR-mediated gene editing experiments.
In vivo: (Z)-4-Hydroxytamoxifen was used at 10mg/Kg orally for the in vivo animal models.

Reference:

  • 1. Jordan VC, et al. A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. (1977) J Endocrinol. 75(2):305-16.
  • 2. 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.
  • 3. 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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