4-Hydroxytamoxifen (E) and (Z) isomers (50:50)

Cell permeable, synthetic estrogen receptor ligand. Widely used in genome engineering. (E) and (Z) isomer mix (50:50).

CreER system:

De facto standard compound in drug-inducible manipulation of CreER recombinase. Allows external temporal control of Cre activity in vivo.

May also be used for TRAPing / in the TRAP / TRAP2 system (Targeted recombination in active populations).

CRISPR/Cas9 gene editing:

Activates an inactived Cas9 nuclease (rendered inactive by insertion of a 4-OHT dependent-intein) to reduce off-target CRISPR-mediated gene editing (once bound with 4-OHT, conditionally active Cas9s modify target genomic sites with ~25-fold higher specificity than wild-type Cas9).

Also allows tight, repeated on-off control of the nuclease activity of the ‘iCas’ Cas9 variant which shows high editing efficiency at multiple loci once bound with 4-OHT.

Pure (Z)-4-hydroxytamoxifen also available.

≥70% Z isomer (remainder primarily E-isomer) 4-Hydroxytamoxifen also available.

Storage of solid

• This compound is light sensitive; exposure to light may affect compound performance. You should therefore store the material in the dark and protect from light.

Storage of solutions

• Do not store the material in solution; make up solutions and use immediately:
• The compound has been shown to isomerise rapidly in solution in most solvents (particulaly solvents with a low dielectric contstant). You should therefore make up and use solutions immediately.
• The isomerisation process can be precluded by storage of the compound at -25°C in the dark as a THF solution containing ca. 0.025% BHT. (Katzenellenbogen et al (1982) J. Org. Chem. 47 2387.)