PROTAC BRD4 Degrader-12

Product Specifications

CAS Number

2417370-90-0

Target

Epigenetic Reader Domain|||PROTAC-Linker Conjugates for PAC|||PROTACs|||Others

Related Pathways

PROTAC|||Chromatin/Epigenetic|||Antibody-drug Conjugate/ADC Related|||Others

Bioactivity

PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC that links von Hippel-Lindau and BRD4 ligands. When conjugated with STEAP1 and CLL1 antibodies, this compound effectively degrades BRD4 protein in PC3 prostate cancer cells, demonstrating potent activity with DC50 values of 0.39 nM and 0.24 nM, respectively [1].

Smiles

CC(OC(=O)O[C@@H]1C[C@H](N(C1)C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)c1cc2N(Cc3c[nH]c4c3c(cn(C)c4=O)-c2cc1CS(C)(=O)=O)c1ncc(F)cc1F)C(C)(C)C)C(=O)NCc1ccc(cc1)-c1scnc1C)C(C)SS(C)(=O)=O