生物活性 | |||
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描述 | NMS-P715 is a selective MPS1 inhibitor with an IC50 of 182 nM. It is highly specific, affecting no kinases below a 5 μM IC50 and only inhibiting CK2, MELK, and NEK6 under 10 μM. NMS-P715 triggers a significant spindle assembly checkpoint (SAC) bypass with an EC50 of 65 nM. At 1 μM, it accelerates mitosis in U2OS cells expressing YFP-α-tubulin, leads to aneuploidy, and suppresses HCT116 cell proliferation. Additionally, NMS-P715 (0.5, 1 μM) impacts the stability of the mitotic checkpoint complex (MCC) and cdc20 ubiquitination[1]. NMS-P715 (1 μM) enables spindle assembly checkpoint bypass and induces apoptosis in pancreatic ductal adenocarcinoma (PDAC) cell lines. Additionally, NMS-P715 (0-25 μM) selectively curtails the growth of PDAC cells[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.48mL 0.30mL 0.15mL |
7.39mL 1.48mL 0.74mL |
14.78mL 2.96mL 1.48mL |
参考文献 |
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