hSMG-1 inhibitor 11j，一种嘧啶衍生物，是有效的和选择性的 hSMG-1 抑制剂，IC50 值为 0.11 nM。hSMG-1 inhibitor 11j 对 hSMG-1 的选择性是 mTOR (IC50=50 nM)，PI3Kα/γ (IC50=92/60 nM) 和 CDK1/CDK2 (IC50=32/7.1 μM) 的 455 倍以上。hSMG-1 inhibitor 11j 可用于癌症研究。
hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα/γ (IC50=92/60 nM) and CDK1/CDK2 (IC50=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer[1].
hSMG-1 inhibitor 11j (0.3-3 μM; 6 h) significantly reduces UPF1 phosphorylation at 0.3 μM, and eliminates it at 1 μM in MDA 361 cells[1].hSMG-1 inhibitor 11j inhibits MDA468 cell proliferation, with an IC50 of 75 nM[1].
参考文献:
[1]. Gopalsamy A, et, al. Identification of pyrimidine derivatives as hSMG-1 inhibitors. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41.
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