MS479

MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: Kd = 200 nM; GLP: Kd = 306 nM) . MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695) ; Blue: GLP ligand (HY-176036) ; Black: linker (HY-176037) ; GLP ligand+linker: HY-176038) [1].

Product Specifications

UNSPSC

12352005

Target

Epigenetic Reader Domain; PROTACs

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

CC1=NN=C2[C@@H](N=C(C3=C(N21)SC(C)=C3C)C4=CC=C(C=C4)Cl)CC(NCCCCCCCCCCNC(CCCN5CCC(NC6=C7C=C(OC)C(OCCCN8CCCC8)=CC7=NC(N9CCOCC9)=C6)CC5)=O)=O

Molecular Formula

C59H82ClN11O5S

Molecular Weight

1092.87

References & Citations

[1]Deng Z, et al., Harnessing the SPOP E3 Ubiquitin Ligase via a Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation. J Med Chem. 2025 Apr 24;68 (8) :8634-8647.