PROTAC BRD2/BRD4 degrader-1

PROTAC BRD2/BRD4 degrader-1

• CAS Number: 2570470-42-5
• 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