1G244 is a potent and selective DPP8/9 inhibitor with IC50 of 14/53 nM and Ki of 0.9/4.2 nM, respectively.
1G244 did not inhibit DPP-IV, FAP, or DPP2 with IC50 value of >100 uM.
1G244 was a slow-tight binding competitive inhibitor of DPP8, but it was a competitive and reversible inhibitor of DPP9.
1G244 blocks adipogenesis in preadipocyte 3T3-L1 and 3T3-F422A, while DPP4 and FAP inhibitors have no effect.
1G244 demonstrated anti-myeloma effects on several cell lines and CD138+ cells from patients as well as in murine xenograft model.
