1G244

• CAT Number: I017434
• CAS Number: 847928-32-9
• Molecular Formula: C₂₉H₃₀F₂N₄O₂
• Molecular Weight: 504.57
• Purity: ≥95%

1G244 (CAT: I017434) is a potent inhibitor of dipeptidyl peptidase 8 (DPP8) and dipeptidyl peptidase 9 (DPP9) with IC50 values of 12 nM and 84 nM, respectively. It exhibits selectivity for DPP8/9 and does not inhibit DPPIV and DPPII. This compound has shown promising pharmacologic actions, inducing apoptosis in multiple myeloma cells and demonstrating anti-myeloma effects. In cell-based experiments, 1G244 treatment dose-dependently decreased the viable cell number of multiple myeloma cell lines. Additionally, it induced apoptosis in MM.1 S cells, as indicated by the detection of cleaved forms of caspase-3 and PARP. In a murine xenograft model, 1G244 treatment suppressed the subcutaneous growth of MM.1 S cells.

Reference

[1]. Sato T, et al. DPP8 is a novel therapeutic target for multiple myeloma. Sci Rep. 2019 Dec 2;9(1):18094.[2]. Leen Heirbaut, et al. Probing for improved selectivity with dipeptidederived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation. MedChemComm. 2016, 7.