1177131-02-0
中文名称
化合物 T25953
英文名称
sodium (E)-4-((3-(4-nitrophenyl)-5-oxo-1-phenyl-4,5-dihydro-1H-pyrazol-4-yl)diazenyl)benzenesulfonate
CAS
1177131-02-0
分子式
C21H14N5NaO6S
分子量
487.421
MOL 文件
1177131-02-0.mol
更新日期
2023/03/20 15:41:17
1177131-02-0 结构式
基本信息
中文别名
化合物 T25953 英文别名
PHPS1 NaPHPS1 Sodium
PHPS-1 Sodium,PHPS1 Sodium
sodium (E)-4-((3-(4-nitrophenyl)-5-oxo-1-phenyl-4,5-dihydro-1H-pyrazol-4-yl)diazenyl)benzenesulfonate
常见问题列表
生物活性
PHPS1 sodium 是一种有效的选择性 Shp2 抑制剂，对 Shp2，Shp2-R362K，Shp1，PTP1B 和 PTP1B-Q 的 Ki 值分别为 0.73，5.8，10.7，5.8 和 0.47 μM。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)
体外研究
PHPS1 (30 μM; 6 days) inhibits proliferation of human tumor cells.
PHPS1 (5-20 μM; 5-360 minutes) inhibits Erk1/2 but not Akt and Stat3 phosphorylation in a dose-dependent manner.
Cell Viability Assay
| Cell Line: | Human cancer cell lines MDA-MB-435, HCT-116 (colon carcinoma), HCT-15 (colon carcinoma), PC-3 (prostate carcinoma), HT-29 (colon carcinoma), NCI-H661 (lung carcinoma), and Caki-1 (kidney carcinoma) |
| Concentration: | 30 μM |
| Incubation Time: | 6 days |
| Result: | Resulted in a reduction in cell number of between 0% (Caki-1) to 74% (HT-29). |
Western Blot Analysis
| Cell Line: | Madin-Darby canine kidney (MDCK) cells |
| Concentration: | 5, 10, 20 μM |
| Incubation Time: | 5, 15, 60, 120, 360 minutes |
| Result: |
Inhibited HGF/SF (1 unit/mL)-induced phosphorylation and thus activation of Erk1/2 over a time period of 15 min to 6 h. In contrast, transient phosphorylation of Erk1/2 after 5 min was not affected.
Exhibited no effect on HGF/SF-induced activation of PI3K/Akt or Stat3. |
体内研究
PHPS1 (3 mg/kg; i.p. injection; every day during the last week on the high-fat diet) renders Ldlr -/- mice less susceptible to atherosclerosis development.
| Animal Model: | Ldlr -/- (005061) mice |
| Dosage: | 3 mg/kg |
| Administration: | Intraperitoneal (i.p.) injection; every day during the last week on the high-fat diet. |
| Result: | Revealed a significant decrease in atherosclerotic plaque size in the aorta compared with the other two groups. |