LD4172 is a first-in-class RIPK1 PROTAC degrader with DC50 values of 4-400 nM in a panel of human and mouse cancer cell lines.
LD4172 is a potent RIPK1 degrader with rapid and sustained effects in vitro.
LD4172 (1 uM) acheives >90% of RIPK1 degradation within 2 and 4 h in Jurkat and B16F10 cells, respectively.
LD4172 sensitizes B16F10 cells to TNFα-mediated apoptosis.
LD4172 induces immunogenic cell death (ICD) and enriches tumor-infiltrating lymphocytes and substantially sensitizes the tumors to anti-PD1 therapy.
