PROTAC BRD2/BRD4 degrader-1

• UNSPSC Description:

  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].

• Target Antigen:

  Epigenetic Reader Domain; PROTACs

• Type:

  Reference compound

• Related Pathways:

  Epigenetics;PROTAC

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/protac-brd2-brd4-degrader-1.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C(NCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCC4=CC5=C(NS(=O)(C6=CC=CC=C6OC)=O)C=CC(N(C)C7=O)=C5C7=C4

• Molecular Weight:

  766.82

• References & Citations:

  [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.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported

• CAS Number:

  2570470-42-5