PROTAC BRD4 Degrader-45 

PROTAC BRD4 Degrader-45 (Compound 2b) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-45 exhibits enhanced passive membrane permeability, stability in cell culture medium supplemented with 10% FBS, and higher intracellular concentrations in cancer cells^[1]. (Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103596); Black: linker).

PROTAC BRD4 Degrader-45 (compound 2b) (10-10000 nM; 4 h) induces BRD4 degradation in MCF-7 cells with a DC₅₀ of 43 nM^[1].
PROTAC BRD4 Degrader-45 (compound 2b) (10 μM; 4 h at 37 °C) has a P_app value of 1.20 in the PAMPA assay, demonstrating moderate passive membrane permeability ^[1].
PROTAC BRD4 Degrader-45 (compound 2b) (1 μM; 30 min at 37 °C (liver microsome assay); 6 h at 37 °C (media stability assay)) shows >90% stability in cell culture media with 10% FBS after 6 h and >90% stability in mouse liver microsomes without NADPH, but undergoes significant metabolism in microsomes with NADPH, with 1.08% remaining^[1].
PROTAC BRD4 Degrader-45 (compound 2b) (10 μM; 0 h, 30 min, 6 h) exhibits superior membrane adsorption and the highest intracellular concentration at 30 min post-treatment in MCF-7 cells^[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]