1G244

Research use only, not for human use.

1G244 is an inhibitor of DPP8/9 with antiatherosclerotic and antimyeloma properties. 1G244 had the IC50 values of 14 and 53 nM against DPP8 and DPP9, and The Ki values for 1G244 were 0.9 and 4.2 nM for DPP8 and DPP9

1G244 is a potent DPP8/9 inhibitor with IC50s 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.

Cell Viability Assay Cell 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 Analysis Cell 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.

Animal Model:NOD/Shi-scid IL-2Rγnull (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.

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Proteasome/Ubiquitin

Proteasome

Proteasome

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847928-32-9

504.57

C29H30F2N4O2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (495.47 mM; Ultrasonic )

N[C@@H](CC(=O)N1CCN(CC1)C(c1ccc(F)cc1)c1ccc(F)cc1)C(=O)N1Cc2ccccc2C1

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(-20℃)

With Ice Pack

≥ 2 years