Dipeptidyl peptidase II (DPPII) is an intracellular protease that localizes to the vesicular system. It releases, preferably at acidic pH, N-terminal dipeptides from oligopeptides with Pro or Ala in the penultimate position. UAMC00039 is a potent reversible competitive tight binding DPPII inhibitor with a Ki of 0.082 nM and an IC50 of 0.48 nM. Both 1 and 100 μM of UAMC00039 inhibited DPPII activity of PBMC and U937 cells more than 90%. UAMC00039 concentrations up to 100 μM were non-toxic for U937 cells for at least 48 h[3]. A dose dependent inhibition of DPPII was observed in the peripheral organs of both the rats and the mice (after oral administration) and the rabbits (after IV administration)[4].
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