For research use only. Not for therapeutic Use.
1G244 (Cat No.: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.
| Catalog Number | I017434 |
| CAS Number | 847928-32-9 |
| Molecular Formula | C₂₉H₃₀F₂N₄O₂ |
| Purity | ≥95% |
| Target | Apoptosis |
| IUPAC Name | (2S)-2-amino-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1-(1,3-dihydroisoindol-2-yl)butane-1,4-dione |
| InChI | InChI=1S/C29H30F2N4O2/c30-24-9-5-20(6-10-24)28(21-7-11-25(31)12-8-21)34-15-13-33(14-16-34)27(36)17-26(32)29(37)35-18-22-3-1-2-4-23(22)19-35/h1-12,26,28H,13-19,32H2/t26-/m0/s1 |
| InChIKey | ZKIQFLSGMMYCGS-SANMLTNESA-N |
| SMILES | C1CN(CCN1C(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)C(=O)C[C@@H](C(=O)N4CC5=CC=CC=C5C4)N |
| Reference | [1]. Sato T, et al. DPP8 is a novel therapeutic target for multiple myeloma. Sci Rep. 2019 Dec 2;9(1):18094.<br>[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. |
