PROTAC BRD4 Degrader-16

PROTAC BRD4 Degrader-16 (compound 7f) potently inhibits BRD4 (BD1) in cell-free HTRF assays with an IC₅₀ of 65.34 nM; it also inhibits BRD4 (BD2) with an IC₅₀ of 27.22 nM. In CCK-8 assays, it potently suppresses the proliferation of MV-4-11 cells with an IC₅₀ value of 12.33 nM^[1].
PROTAC BRD4 Degrader-16 (10-1000 nM; 4-24 h) induces sustained degradation of BRD2, BRD3, BRD4 L and BRD4 S, and downregulates c-Myc in MV-4-11 cells, with no recovery of BRD4 S expression observed at 24 h^[1].
PROTAC BRD4 Degrader-16 (100 nM; 0-24 h) mediates sustained and complete degradation of BRD4 L and BRD4 S in MV-4-11 cells within 12 h via the ubiquitin-proteasome system, with no rebound of BRD4 S expression observed^[1].
PROTAC BRD4 Degrader-16 generates truncated form 7f_cut, which binds to the BRD4 BD2 domain via hydrogen bonds and π-π interactions, with an overall MM/GBSA binding energy of -49.0 kcal/mol^[1].
PROTAC BRD4 Degrader-16 (100 nM; 24 h) can induce G0/G1 cell cycle arrest in MV-4-11 cells by upregulating p21 and downregulating CDK4 at a concentration of 100 nM for 24 h; it only induces a small number of apoptosis in MV-4-11 cells, and no Mcl-1 downregulation or PARP cleavage was detected^[1].

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