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。
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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].
[1]. Sato T, et al. DPP8 is a novel therapeutic target for multiple myeloma. Sci Rep. 2019 Dec 2;9(1):18094. [2]. Leen Heirbaut, et al. Probing for improved selectivity with dipeptidederived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation. MedChemComm. 2016, 7.
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