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1177131-02-0

中文名稱 化合物 T25953
英文名稱 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 結(jié)構(gòu)式 1177131-02-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T25953
英文別名
PHPS1 Na
PHPS1 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

物理化學(xué)性質(zhì)

形態(tài)Solid
顏色Brown to reddish brown

常見問題列表

生物活性
PHPS1 sodium 是一種有效的選擇性 Shp2 抑制劑,對 Shp2,Shp2-R362K,Shp1,PTP1B 和 PTP1B-Q 的 Ki 值分別為 0.73,5.8,10.7,5.8 和 0.47 μM。
靶點

Ki: 0.73 μM (Shp2), 5.8 μM (Shp2-R362K), 10.7 μM (Shp1), 5.8 μM (PTP1B), 0.47 μM (PTP1B-Q)

體外研究

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.
體內(nèi)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.
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