DG013A

DG013A is a moderate inhibitor of ERAP1 and ERAP2, but acts as a highly potent inhibitor of the off-target M1-aminopeptidase APN (IC₅₀ = 0.0037 μM)^[1].
DG013A exhibits negligible passive permeability in Caco-2 cells, which is inconsistent with its use as a convertible intracellular chemical probe^[1].
DG013A is a potent nanomolar ERAP1 inhibitor (IC₅₀ = 33 nM) and ERAP2 inhibitor (IC₅₀ = 11 nM), and it also inhibits IRAP and APN, with its binding to ERAP2 involving coordination of its phosphonic acid group with the active-site zinc ion^[2].
DG013A is a potent inhibitor of recombinant ERAP1 with an IC₅₀ of 43.5 nM^[3].
DG013A shows weak antiproliferative activity in HCT116 cells, possibly due to off-target effects^[1].
DG013A (0-30 μM; 48 h) shows no toxicity toward A375 malignant melanoma cells at concentrations up to 30 μM for 48 h^[3].
DG013A modulates antigen presentation and the immunopeptidome in HeLa-B27, CT26, and melanoma cells^[2].
DG013A (1 μM; 6 days) does not significantly alter cell surface MHC-I levels in A375 malignant melanoma cells within 6 days^[3].
DG013A (18-22 h) inhibits ERAP1-dependent SIINFEKL epitope antigen presentation in H-2 K^b-expressing HeLa cells with an apparent ED₅₀ of 350 nM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.