2007955-07-7

DG013A is a a phosphinic pseudotripeptide and ERAP2 inhibitor with nanomolar potency for ERAP2. A crystal structure of a phosphinic pseudotripeptide (DG013A) bound into the active site of ERAP2 revealed five distinct protein elements that were hypothesized to drive inhibitor potency.

DG013A?is a phosphinic acid tripeptide mimetic inhibitor. DG013A displays significantly weak affinity for both ERAP1 (IC50=33?nM)?and ERAP2 (IC50=11?nM). DG013A can be used for the research of autoimmune disease and cancer[1].

[1] Birgit Wilding,?et al. Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1. Bioorg Med Chem Lett.?2021 Jun 15;42:128050. DOI:10.1016/j.bmcl.2021.128050