FLIPinB is a first-in class, specific small molecule inhibitor of c-FLIPL in the caspase-8/c-FLIPL heterodimer, promotes CD95L- and TRAIL-mediated loss of cell viability and cell death.
FLIPinB enhances CD95L-/TRAIL-mediated loss of cell viability in Jurkat, HeLa-CD95 and HeLa-CD95-FL cells, increases caspase activation.
Co-treatment with FLIPinBγ increased the rate of CD95L-induced apoptotic cell death in HeLa-CD95-FL cells.
FLIPinB sensitizes the cell death in pancreatic cancer cells induced by combinatorial treatment with Death Ligand (DL), gemcitabine and Mcl-1 inhibitor S63845.
c-FLIPL, the long isoform of c-FLIP, is a DED-containing protein and a key regulator of the extrinsic apoptosis pathway. DISC comprises DR, FADD, procaspase-8/10 and c-FLIPL/S/R proteins,  DISC serves as a platform for procaspase-8 activation, which takes place upon its oligomerization in the death effector domain (DED)-filaments, initiating the apoptotic destruction of the cell.