PROTAC BRD2/BRD4 degrader-1 

PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A^[1].

PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC₅₀ value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells^[1].
PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC₅₀ value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells^[1].
PROTAC BRD2/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours) induces MV4-11 apoptosis lines^[1].
PROTAC BRD2/BRD4 degrader-1 exhibits excellent anti-proliferative activity in 6 leukemia cell lines of NCI. Among them, the GI₅₀ values of the three leukemia cell lines were lower than 50 nM, consistent with the activity of leukemia MV4-11 cells^[1].
PROTAC BRD2/BRD4 degrader-1 has good anti-proliferation activity including prostate Cancer (22RV1 IC₅₀: 0.081 μM), colon cancer (colo-205 IC₅₀: 0.1557 μM) and thyroid cancer(TT IC₅₀: 0.037451 μM)^[1].

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

766.82

C₃₉H₃₈N₆O₉S

2570470-42-5

Room temperature in continental US; may vary elsewhere.

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

• [1]. Jiang F, et al. Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2019 Nov 11:115181.  [Content Brief]