(Z)-4-Hydroxytamoxifen --- CRISPR Editing Enhancer

(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.

Product information

CAS Number: 68047-06-3

Molecular Weight: 387.51

Formula: C26H29NO2

Synonym:

4-OH-TAM

4-OHT

Afimoxifene

4-Hydroxytamoxifen

(Z)-4-Hydroxytamoxifen

Hydroxytamoxifen

Tamogel

Related CAS Number:

164365-20-2

Chemical Name: (Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol

Smiles: CC/C(=C(\C1C=CC(O)=CC=1)/C1C=CC(=CC=1)OCCN(C)C)/C1C=CC=CC=1

InChiKey: TXUZVZSFRXZGTL-QPLCGJKRSA-N

InChi: InChI=1S/C26H29NO2/c1-4-25(20-8-6-5-7-9-20)26(21-10-14-23(28)15-11-21)22-12-16-24(17-13-22)29-19-18-27(2)3/h5-17,28H,4,18-19H2,1-3H3/b26-25-

Technical Data

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: 4^oC for 1 year, -20^oC for 3years. DMSO: 4^oC 3 month.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4^oC for short term (days to weeks), or -20^oC for long term (months).

Drug Formulation: This drug may be formulated in DMSO

HS Tariff Code: 2934.99.9001

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.

References:

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.