PROTAC BRD4 Degrader-21

PROTAC BRD4 Degrader-21 (compound 074) (40 μM to 2.0 nM) binds to recombinant HSP90α protein with moderate affinity, having an IC₅₀ of 100-1000 nM in a fluorescent polarization assay^[1].
PROTAC BRD4 Degrader-21 (10 μM; 1 hr) binds specifically to bromodomains of the BET family proteins, showing strong competition for ligand binding to BRD2, BRD3, BRD4, and BRDT bromodomains at 10 μM, while displaying minimal binding to non-BET bromodomains^[1].
PROTAC BRD4 Degrader-21 (40 μM to 2.0 nM; 2 hr) binds to recombinant BRD4 (BD1+BD2) protein with moderate affinity, having an IC₅₀ of 100-1000 nM in a homogeneous time resolved fluorescence assay^[1].
PROTAC BRD4 Degrader-21 (100-300 nM; 24 hr) induces degradation of BRD4 protein in MV4-11 acute myeloid leukemia cells when treated at 100 nM and 300 nM for 24 hr^[1].
PROTAC BRD4 Degrader-21 (24 hr) reduces MYC protein expression in MV4-11 acute myeloid leukemia cells with an IC₅₀ <100 nM after 24 hr of treatment^[1].
PROTAC BRD4 Degrader-21 selectively degrades BRD4 over HSP90 client proteins, with its IC₅₀ for BRD4 degradation (59 nM in MV4-11 cells) being 6- to 18-fold lower than its IC₅₀ values for degradation of ERBB2, IGF1R, EGFR, and RAF1^[1].
PROTAC BRD4 Degrader-21 (72 hr) potently inhibits the growth of MV4-11 acute myeloid leukemia cells, with an IC₅₀ <100 nM in a 72-hr CCK-8 cytotoxicity assay^[1].
PROTAC BRD4 Degrader-21 degradates HSP90 client proteins, with IC₅₀ values of 340 nM, 1055 nM, 405 nM, 762 nM for ERBB2, IGF1R, EGFR and RAF1, respectively^[1].

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