| 产品描述: | 一种可渗透细胞的磷酸酪氨酸类似物,可作为Shp-2的活性位点靶向抑制剂。;A cell-permeable phosphotyrosine analog that can be used as an active site-targeting inhibitor of Shp-2.;PTP抑制剂V,PHPS1是一种可渗透细胞的磷酸酪氨酸类似物,可作为可逆的,以活性位点为靶点,与底物竞争的Shp-2抑制剂(IC | 50 |和K | i | = 2.1和0.73 µM)。PHPS1仅在较高浓度(IC | 50 | 分别为5.4、19、30和39 µM)下抑制ECPTP,PTP1B,Shp1,分枝杆菌MptpA,甚至对PTPH1,STEP,PTPN7,PTPRK,GLEPP1或LAR2几乎没有活性。浓度高达50 µM。PTP抑制剂V,PHPS1已被证明抑制Shp-2依赖性细胞信号传导和肿瘤细胞集落的形成。;PTP inhibitor V, PHPS1 is a cell-permeable phosphotyrosine analogue, which can be used as a reversible, active site as a target, and a Shp-2 inhibitor that competes with the substrate (IC | 50 | and K | i | = 2.1 and 0.73 µM). PHPS1 inhibits ECPTP, PTP1B, Shp1, Mycobacterium MptpA only at higher concentrations (IC | 50 | 5.4, 19, 30, and 39 µM, respectively), and even almost none against PTPH1, STEP, PTPN7, PTPRK, GLEPP1 or LAR2 active. Concentrations up to 50 µM. PTP inhibitor V, PHPS1 has been shown to inhibit Shp-2-dependent cell signal transduction and tumor cell colony formation.
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| 靶点: |
Ki: 0.73 μM (Shp2), 5.8 μM (Shp2-R362K), 10.7 μM (Shp1), 5.8 μM (PTP1B), 0.47 μM (PTP1B-Q) |
| 体内研究: |
PHPS1 (3 mg/kg;i.p.;高脂肪饮食的最后一周的每一天) 使 Ldlr-/- 小鼠不易发生动脉粥样硬化。 |
| 参考文献: |
1. Klaus Hellmuth, et al. Specific Inhibitors of the Protein Tyrosine Phosphatase Shp2 Identified by High-Throughput Docking. Proc Natl Acad Sci U S A. 2008 May 20;105(20):7275-80. 2. Jia Chen, et al. SHP2 Inhibitor PHPS1 Protects Against Atherosclerosis by Inhibiting Smooth Muscle Cell Proliferation. BMC Cardiovasc Disord. 2018 Apr 27;18(1):72. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.148 ml |
10.742 ml |
21.485 ml |
| 5 mM |
0.43 ml |
2.148 ml |
4.297 ml |
| 10 mM |
0.215 ml |
1.074 ml |
2.148 ml |
| 50 mM |
0.043 ml |
0.215 ml |
0.43 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |