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• 产品描述： ML364是去泛素化酶USP2的小分子抑制剂，IC50为1.1 μM（以含内部淬灭荧光双泛素为底物）

• 靶点： USP8(Cell-free assay):0.95 μM; USP2(Cell-free assay):1.1 μM;DUB

• 体外研究：
  ML364 induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest in Mino and HCT116 cancer cell lines. ML364 is antiproliferative in cancer cell lines. ML364 also causes a decrease in homologous recombination-mediated DNA repair. It is inactive against caspase 6, caspase 7, MMP1, MMP9, and USP15, but does inhibit USP8 with an IC50 of 0.95 μM. In a panel of 102 kinases that included regulators of the cell cycle there is no binding observed to any of the enzymes tested using 10 μM ML364.

• 细胞实验： Cell lines: LnCAP cells and MCF7 cells Concentrations: 0-20 μM Incubation Time: 24 h Method: ML364 promotes degradation of cyclin D1 in LnCAP cells and MCF7 cells. Cells are treated with ML364 for 24 h, and cyclin D1 protein levels are assessed by Western blotting using a tubulin control.

• 参考文献：
  1. Davis MI, et al. Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models. J Biol Chem. 2016, 291(47):24628-24640..

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.932 ml	9.661 ml	19.322 ml
  5 mM	0.386 ml	1.932 ml	3.864 ml
  10 mM	0.193 ml	0.966 ml	1.932 ml
  50 mM	0.039 ml	0.193 ml	0.386 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *