Gossypetin-DataSheet-生命科学试剂-MedChemExpresss

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGossypetinCat. No.: HY-119917CAS No.: 489-35-0分式: CHO分量: 318.24作靶点: p38 MAPK作通路: MAPK/ERK Pathway储存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 Gossypetin六羟化的类酮，种有效的 MKK3 和 MKK6 抑

2、制剂，可强烈减弱 MKK3/6-p38 信号传导途径，具有多种药理活性，包括抗氧化，抗和抗癌活性。IC50 & Target p38 MAP kinase体外研究Gossypetin (20-60 M; 48 hours; KYSE30, KYSE450 and KYSE510 cells) treatment significantly inhibitsanchorage-dependent esophageal cancer cell growth in dose dependent manner. Gossypetin stronglysuppresses anchorage-indep

3、endent cell growth in esophageal cancer cells 1.Gossypetin (60 M; 3 hours; KYSE30 and KYSE410 cells) treatment strongly inhibits p38 activity in a dose-dependent manner and confirms that Gossypetin directly suppresses MKK3 or MKK6 activity 1.Gossypetin (20-40 M; 48 hours; KYSE450 and KYSE510 cells)

4、treatment reduces S phase and induces G2phase cell cycle arrest in a dose-dependent manner 1.Gossypetin (20-40 M; 72 hours; esophageal cancer cells) treatment induces intrinsic apoptosis ofesophageal cancer cells 1.Cell Proliferation Assay 1Cell Line: KYSE30, KYSE450 and KYSE510 cellsConcentration:

5、20 M, 40 M, 60 MIncubation Time: 48 hoursResult: Anchorage-dependent esophageal cancer cell growth was significantly inhibited.1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEWestern Blot Analysis 1Cell Line: KYSE30 and KYSE410 ccellsConcentration: 60 MIncubation Time: 3 hoursResult: p38 activity w

6、as strongly inhibited in a dose-dependent manner.Cell Cycle Analysis 1Cell Line: KYSE450 and KYSE510 cellsConcentration: 20 M, 40 MIncubation Time: 48 hoursResult: Reduced S phase and induces G2 phase cell cycle arrest in a dose-dependent manner.Apoptosis Analysis 1Cell Line: Esophageal cancer cells

7、Concentration: 20 M, 40 MIncubation Time: 72 hoursResult: Induced apoptosis of esophageal cancer cells.体内研究 Gossypetin (100 mg/kg; oral administration; 5 times per week; for 21 days; severe combinedimmunodeficiency (SCID) female mice) treatment significantly decreases the volume of esophageal tumorg

8、rowth and without significant loss of body weight. The expression of Ki67 is significantly decreased byGossypetin. There are no obvious morphological differences between tissues from treated or untreated mic.The phosphorylation of p38, the direct downstream protein of MKK3/6 strongly inhibited in th

9、e Gossypetin-treated group 1.Animal Model: Severe combined immunodeficiency (SCID) female mice (6-9 weeks old) injection withesophageal cancer tissue 1Dosage: 100 mg/kgAdministration: Oral administration; 5 times per week; for 21 daysResult: Suppressed patient-derived esophageal xenograft tumor grow

10、th in an in vivo mousemodel.REFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Xie X, et al. Gossypetin is a novel MKK3 and MKK6 inhibitor that suppresses esophageal cancer growth in vitro and in vivo. Cancer Lett.2019 Feb 1;442:126-136.McePdfHeightCaution: Product has not been fully valida