Drug intelligence / Profile preview

4-hydroxycyclofen

Development stage
Unknown
Modality
Small Molecules
01

Overview

4-Hydroxycyclofen (also known as cyclofen-OH or 4-OHC) is a synthetic, photostable analog of 4-hydroxytamoxifen (4-OHT). It acts as a potent estrogen receptor (ER) ligand. It is widely used in optochemogenetics and chemical biology as a ligand to control the activity of proteins fused to a mutated estrogen receptor ligand-binding domain (such as Cre-ERT2 or Cas9-ERT2). When caged with photolabile protecting groups (such as DMNPE or Cy7 derivatives), its activity is masked until light-induced uncaging (photo-uncaging) releases the active 4-hydroxycyclofen, enabling precise spatiotemporal control of gene recombination (via Cre/LoxP) or gene editing in vitro and in vivo.

Other names
4-OHCcyclofen-OH
02

Targets

ER (Estrogen receptor)

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