Pomalidomide-amido-C1-Br

Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity[1].

Research Areas >> Cancer

Signaling Pathways >> PROTAC >> E3 Ligase Ligand-Linker Conjugate

Cereblon

Pomalidomide-amido-C1-Br (Compound 6) can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (Compound 2). PROTAC B-Raf degrader 1 can effectively kill cancer cells via inducing cells apoptosis. As a B-Raf degrader, PROTAC B-Raf degrader 1 can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf[1].

[1]. Chen H, et al. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation. Bioorg Chem. 2019 Jun;87:191-199.