NMS-859 - p97 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENMS-859Cat. No.: HY-15714CAS No.: 1449236-96-7分式: CHClNOS分量: 349.79作靶点: p97作通路: Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 42 mg/mL (120.07 mM)* means soluble, but

2、 saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8589 mL 14.2943 mL 28.5886 mL5 mM 0.5718 mL 2.8589 mL 5.7177 mL10 mM 0.2859 mL 1.4294 mL 2.8589 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NMS-859种有效的，共价的 VCP (p97) 抑制剂，细胞中分别在 60 M 和 1 mM ATP 的条件下，对野型V

3、CP 的 IC50 值分别为 0.37 和 0.36 M。IC50 & Target IC50: 360 nM (Cellular p97, 1 mM ATP), 370 nM (Cellular p97, 60 M ATP) 1体外研究NMS-859 is a potent VCP inhibitor, with IC50s of 0.37 and 0.36 M for wild-type VCP in the presence of 60 1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEM and 1 mM ATP in cells, re

4、spectively. NMS-859 shows very weak inhibitory activity against VCPC522T.NMS-859 also suppresses the proliferation of cells, with IC50s of 3.5 M and 3.0 M in HCT116 and HeLacell lines, respectively 1.PROTOCOLCell Assay 1 Cells are seeded at 1,600 cells per well in 384-well white clear-bottom plates.

5、 Twenty-four hours afterseeding, cells are treated with NMS-859 (eight dilution points, in duplicate) and incubated for an additional 72h at 37C under a 5% CO2 atmosphere. Cells are then lysed, and the ATP content in each well is determinedusing a thermostable firefly luciferase-based assay as a mea

6、sure of cell viability. IC50 values are calculatedusing the percentage of growth of treated cells versus the untreated control 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Magnaghi P, et al. Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. Nat Chem Biol. 2013Sep;9(9):548-56.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel