LD4172

LD4172 is a PROTAC degrader capable of degrading RIP kinase (RIPK1) with a DC50 in the nanomolar range. When used in combination with TNF-α, LD4172 can induce apoptosis in B16F10 cells. In mouse models, it demonstrates antitumor activity. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase VHL)

NC1=C2C(=CN(CCCNC(CCCCCCCCCCC(N[C@H](C(=O)N3[C@H](C(N[C@@H](C)C4=CC=C(C=C4)C=5SC=NC5C)=O)C[C@@H](O)C3)[C@](C)(C)C)=O)=O)C2=NC=N1)C=6C=C7C(=CC6)N(C(CC8=CC(OC(F)(F)F)=CC=C8)=O)CC7