NMS-859 is a potent and specific small molecule covalent inhibitor of theATPase VCP/p97 (IC50 ~0.37 μM), identified by high-throughput screening.
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NMS-859 is a potent VCP inhibitor, with IC50s of 0.37 and 0.36 μM against wild-type VCP in the presence of 60 μM and 1 mM ATP in cellular contexts, respectively. It exhibits minimal inhibitory action against VCPC522T mutation. NMS-859 also inhibits cell proliferation, with IC50 values of 3.5 μM for HCT116 cells and 3.0 μM for HeLa cells[1].
体外研究
NMS-859 is a potent VCP inhibitor, with IC50s of 0.37 and 0.36 μM against wild-type VCP in the presence of 60 μM and 1 mM ATP in cellular contexts, respectively. It exhibits minimal inhibitory action against VCPC522T mutation. NMS-859 also inhibits cell proliferation, with IC50 values of 3.5 μM for HCT116 cells and 3.0 μM for HeLa cells[1].
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