1G244

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

1G244 是一种有效的 DPP8/9 抑制剂，IC50 分别为 12 nM 和 84 nM，但不抑制 DPPIV 和 DPPII。1G244 可诱导多发性骨髓瘤细胞凋亡，并具有抗骨髓瘤作用。

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 中的溶解度 : 250 mg/mL (495.47 mM; 超声助溶 )

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