CCF642 (CCF 642) is a novel covalent protein disulfide isomerase (PDI) inhibitor with IC50 of 2.9 uM, shows antimyeloma activity.
CCF642 inhibits PDI reductase activity about 100-fold more potently than PACMA 31 and LOC14.
CCF642 shows cytotoxicity against MM cells with a submicromolar IC50, causes acute ER stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release.
CCF642 displays potent efficacy and prolongs the lifespan in an aggressive syngeneic mouse model of multiple myeloma.
