1G244 (C09-1135-552)

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 effectsIn Vitro1G244 (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. ?/n1G244 (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 Vivo1G244 (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:SolidIC50& Target:DPP-4. Specification: 0.98 Molecular Formula: C29H30F2N4O2 Molecular Weight: 504.57 PubChem CID: 56658139 Isomeric 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