BDM88951 (BDM 88951) is a highly potent, selective inhibitor of endoplasmic reticulum aminopeptidase 2 (ERAP2) with IC50 of 19 nM.
BDM88951 displays selectivity index (>150) towards closely related ERAP1 and IRAP enzymes, as well as MMPs, TACE and LAP3.
BDM88951 is a potent inhibitor of ERAP2-mediated hydrolysis of two nonapeptides precursors of SIINFEKL, an ovalbumine-derived antigen, in a
dose dependent manner.
BDM88951 engage ERAP2 in cells and inhibits antigen presentation in a cellular context, also displays favorable in vitro ADME properties and in vivo exposure.
