1G244

1G244 is a potent DPP8/9 inhibitor with IC 50 s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects In Vitro 1G244 (0-100 μM; 72 hours; Delta47, U266 , KMS-5, RPMI8226, or MM.1?S cells) treatment dose-dependently decreases viable cell number of five multiple myeloma cell lines. ? 1G244 (50 μM; 0-48 hours; MM.1?S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells Concentration: 0 μM, 1 μM, 5 μM, 10 μM, 50 μM, or 100 μM Incubation Time: 72 hours Result: Dose-dependently decreased viable cell number of five multiple myeloma cell lines. Western Blot AnalysisCell Line: MM.1 S cells Concentration: 50 μM Incubation Time: 0 hour, 3 hours, 6 hours, 12 hours, 24 hours, 48 hours Result: Decreased caspase-3 and PARP protein. In Vivo 1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1?S cells in murine xenograft model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD/Shi-scid IL-2Rγ (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells Dosage: 30 mg/kg Administration: Subcutaneous injection; once-a-week; for 3 weeks Result: Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model. Form:Solid IC50& Target:DPP-4

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet