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[1][2].

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[1]. 1G244 (50 μM; 0-48 hours; MM.1?S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected[1].

In murine xenograft model, 1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks;) treatment significantly suppresses the subcutaneous growth of MM.1?S cells [1].

847928-32-9

C29H30F2N4O2

504.57

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years