1G244

1G244 is an inhibitor of dipeptidyl peptidase 8 (DPP-8) and DPP-9 (IC₅₀s = 14 and 53 nM, respectively).¹ It is selective for DPP-8 and DPP-9 over DPP-4, DPP-2, and fibroblast activation protein (FAP; IC₅₀s = >100 µM for all). 1G244 (20 µM) inhibits the differentiation of 3T3-L1 cells into adipocytes.² It induces caspase-1-dependent pyroptosis in RAW 264.7 macrophages when used at a concentration of 10 µM.³ 1G244 (2 mg/kg) decreases atherosclerotic lesion area and M1-like macrophage plaque infiltration in apoE^-/- mice in a model of atherosclerosis induced by a high-fat diet.⁴

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1. Wu, J.J., Tang, H.K., Yeh, T.K., et al. Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor. Biochem. Pharmacol. 78(2), 203-210 (2009).

2. Han, R., Wang, X., Bachovchin, W., et al. Inhibition of dipeptidyl peptidase 8/9 impairs preadipocyte differentiation. Sci. Rep. 5(12348), 1-11 (2015).

3. Okondo, M.C., Johnson, D.C., Sridharan, R., et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat. Chem. Biol. 13(1), 46-53 (2017).

4. Wiśniewska, A., Czepiel, K., Stachowicz, A., et al. The antiatherosclerotic action of 1G244 - An inhibitor of dipeptidyl peptidases 8/9 - is mediated by the induction of macrophage death. Eur. J. Pharmacol. 944, 175566 (2023).