| 货号 | 16615-1mg |
| 描述 | BVT 948 is a noncompetitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTP; IC50s = 0.09-1.7 µM).1 It facilitates the oxidation of the catalytic cysteine residue by hydrogen peroxide.1 Similarly, it inhibits redox-sensitive cytochrome P450 (CYP) isoforms, including CYP2C19 and CYP2D6, with IC50 values less than 10 µM.1 BVT 948 also inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3 with IC50 values from 0.7 to 3.2 µm.2 Presumably through its effects on PTPs, BVT 948 enhances insulin signaling in cells and insulin tolerance in ob/ob mice, suppresses the expression of matrix metalloproteinase-9 and invasion in breast cancer cells, and increases NMDA-induced substance P release by spinal cord slices.1,3,4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Liljebris, C.,Baranczewski, P.,Björkstrand, E., et al. Oxidation of protein tyrosine phosphatases as a pharmaceutical mechanism of action: A study using 4-hydroxy-3,3-dimethyl-2H-benzo[g]indole-2,5(3H)-dione. Journal of Pharmacology and Experimental Therapeutics 309(2), 711-719 (2004). 2.Blum, G.,Ibáñez, G.,Rao, X., et al. Small-molecule inhibitors of SETD8 with cellular activity. ACS Chemical Biology 9(11), 2471-2478 (2014). 3.Hwang, B.M.,Chae, H.S.,Jeong, Y.J., et al. Protein tyrosine phosphatase controls breast cancer invasion through the expression of matrix metalloproteinase-9. BMB Rep. 46(11), 533-538 (2013). 4.Chen, W.,Zhang, G. and Marvizón, J.C.G. NMDA receptors in primary afferents require phosphorylation by Src family kinases to induce substance P release in the rat spinal cord. Neuroscience 166(3), 924-934 (2010). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 241.2 |
| 分子式 | C14H11NO3 |
| CAS号 | 39674-97-0 |
| 稳定性 | ≥ 2 years |
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