货号	规格	价格	上海	北京	珠海	重庆	武汉
S89265-5mg买3赠1	99.90%	￥420.00 S89265-5mg ￥420.00 现货（买3赠1）	5 5	-	-	-	-
S89265-10mg促销	99.90%	￥600.00 ￥480.00 S89265-10mg ￥480.00 现货	5 5	-	-	-	-
S89265-25mg促销	99.90%	￥710.00 ￥568.00 S89265-25mg ￥568.00 现货	3 3	-	-	-	-
S89265-100mg	≥98%	￥1870.00 S89265-100mg ￥1870.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

PHPS1 (PTP Inhibitor V) 是一种有效的细胞渗透性抑制剂，对 Shp2 具有特异性，Ki 值为 0.73 μM

靶点：

Shp2(Cell-free assay):0.73 μM(Ki);Phosphatase

体外研究：

PHPS1 inhibits Shp2-dependent cellular events such as hepatocyte growth factor/scatter factor (HGF/SF)-induced epithelial cell scattering and branching morphogenesis. PHPS1 also blocks Shp2-dependent downstream signaling, namely HGF/SF-induced sustained phosphorylation of the Erk1/2 MAP kinases and dephosphorylation of paxillin. Furthermore, PHPS1 efficiently inhibits activation of Erk1/2 by the leukemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumor cell lines

体内研究：

PHPS1 decreases the number of atherosclerotic plaques without significantly affecting body weight, serum glucose levels or lipid metabolism. Plaque composition analysis shows a significant decrease in the number of VSMCs in atherosclerotic lesions of Ldlr−/− mice treated with PHPS1. Stimulation with oxLDL induces a dose-dependent increase in the number of VSMCs and in SHP2 and ERK phosphorylation levels, and these effects are blocked by PHPS1

细胞实验：

Cell lines: MDCK cells, NIH 3T3 cells, HEK293 cells Concentrations: 10 μM, 20 μM Incubation Time: 2 days Method: MDCK cells are either untreated or treated with 20 μM PHPS1 and stimulated with 1 unit/ml of HGF/SF. Paxillin is immunoprecipitated from total cell lysates and immunoblotted with antibodies specific for paxillin and for phosphotyrosine. NIH 3T3 cells are transfected with an expression vector for RasV12 and either untreated or treated with 10 μM PHPS1 for 2 days, respectively. Total cell lysates are immunoblotted with antibodies specific for phospho-Erk1/2 (P-Erk1/2) and Erk1/2. HEK293 cells are transfected with expression vectors for HA-GAB2, HA-SHP2-E76K, or ERBB2 and either untreated or treated with 20 μM PHPS1. Total cell lysates are immunoblotted with antibodies specific for hemagglutinin epitope (HA), phospho-Erk1/2 (P-Erk1/2), and Erk1/2.

动物实验：

Animal Models: Ldlr−/− mice Dosages: 3 mg/kg Administration: i.p.

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.

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	2.052 ml	10.258 ml	20.516 ml
5 mM	0.41 ml	2.052 ml	4.103 ml
10 mM	0.205 ml	1.026 ml	2.052 ml
50 mM	0.041 ml	0.205 ml	0.41 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。

参考文献

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