PROTAC BRD4 Degrader-44 

PROTAC BRD4 Degrader-44 (compound 2a) is a PROTAC degrader targeting BRD4 with passive membrane permeability. PROTAC BRD4 Degrader-44 maintains stability within 6 hours in medium supplemented with 10% FBS. PROTAC BRD4 Degrader-44 shows a trend of increasing intracellular accumulation within 6 hours, indicating reduced efflux^[1]. (Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103596); Black: linker).

PROTAC BRD4 Degrader-44 (compound 2a) (10-10000 nM; 4 h) potently degrades BRD4 in MCF-7 cells with a DC₅₀ of 16 nM^[1].
PROTAC BRD4 Degrader-44 (compound 2a) (1 μM; 30 min/6 h at 37 °C) shows high stability in culture medium with 10% FBS and moderate stability in mouse liver microsomes in the absence of NADPH, with 1.70% compound remaining after 30 min in the presence of NADPH^[1].
PROTAC BRD4 Degrader-44 (compound 2a) (10 μM; 0 h, 30 min, 6 h at 37 °C) accumulates in MCF-7 cells, with higher intracellular concentrations than dBET1 at all measured time points, and comparable levels to diastereomer after 6 h of incubation^[1].

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

800.28

C₃₉H₃₈ClN₇O₈S

CC1=C(SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@H](C4=NN=C(N24)C)CC(O[C@@H](CCC(NCCOC5=CC=CC(C6=O)=C5C(N6C7C(NC(CC7)=O)=O)=O)=O)C)=O)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Abdelwahid MAS, et al. Diastereomeric Branched-Ester dBET1 Analogs Exhibit Conformation-Dependent Differences in Passive Membrane Permeability. J Med Chem. 2026;69(3):2900-2915.  [Content Brief]