BRD4 degrader-6 is a dimeric BDR4PROTAC class degrader with a DC50 of less than 0.1 μM. It effectively induces the ubiquitination and degradation of BDR4, exhibiting anticancer properties.

BRD4:<0.1 μM(DC50)

BRD4 degrader-6 (example 1) is effective in degrading BRD4 in BRD4 HiBiT cells, with a DC₅₀ of less than 0.11 μM, following a pretreatment of 1.5 nM for 2 hours and an additional treatment for 24 hours. The compound relies on the reversibility of its bonds to dissociate into monomers both in vitro and in vivo, allowing cellular entry, subsequent reformation into dimers within the cells, and subsequent binding to the target protein, which leads to ubiquitin-proteasome degradation of the target protein.