PROTAC BRD4 Degrader-1 

PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC₅₀ of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression^[1].

PROTAC BRD4 Degrader-1 (compound 21) (2.5 μM; 24 hours) shows high inhibitory activity against the growth of human monocyte lymphoma cell line THP-1, with the IC₅₀ value of 0.81 μM, and moderate activity against Raji and HL-60 cell lines^[1].
PROTAC BRD4 Degrader-1 (1 μM; 24 hours) effectively induces the degradation of BRD4 protein and suppression of c-Myc, while pomalidomide couldn’t degrade BRD4 at the low concentration^[1].

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

771.78

C₄₀H₃₇N₉O₈

2133360-00-4

O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)COCCN4N=NC(CN5C(N(C)C6=C(C=C(C7=C(C)ON=C7C)C=C6)C5C8=CC=CC=C8)=O)=C4

Room temperature in continental US; may vary elsewhere.

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

• [1]. Zhang F, et al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.Bioorg Med Chem. 2020 Jan 1;28(1):115228.  [Content Brief]