CFT-743

CFT-743 binds tightly to both purified BRD4 BD1 and purified CRBN-DDB1 complex, with minimal cooperative effects between the two proteins during ternary complex formation^[1].
CFT-743 drives ternary complex formation between purified BRD4 BD1 and purified CRBN-DDB1 with high affinity, and exhibits minimal protein-protein cooperativity in this complex^[1].
CFT-743 (3-1000 nM; 30-90 min) induces low-rate ubiquitination of purified HA-tagged BRD4 BD1 in HeLa cell-free lysates, with tight binding to BD1 and moderate binding to CRBN, following an essential activator kinetic model^[1].
CFT-743 (10 µM down to serially diluted half-log concentrations; 3 h) induces minimal degradation of HiBiT-tagged BRD4 BD1 in 293T cells, with a DC₅₀ of 4.3 nM and very low maximal efficacy^[1].
CFT-743 (30-3000 nM; 30-90 min) induces low-rate ubiquitination of endogenous BRD4 in HeLa cell-free lysates, with a slower maximal velocity compared to purified BRD4 BD1 due to lower endogenous target concentration^[1].
CFT-743 preferentially induces diubiquitination of purified HA-tagged BRD4 BD1 in HeLa cell-free lysates, unlike other tested BiDACs that predominantly induce monoubiquitination^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.