Chrysophanol-Chrysophanic-acid-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEChrysophanolCat. No.: HY-13595CAS No.: 481-74-3Synonyms: Chrysophanic acid分式: CHO分量: 254.24作靶點: EGFR作通路: JAK/STAT Signaling; Protein Tyrosine Kinase/RTK儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體

2、外實驗 DMSO : 2 mg/mL (7.87 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.9333 mL 19.6665 mL 39.3329 mL5 mM 0.7867 mL 3.9333 mL 7.8666 mL10 mM - - -請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Chrysophanol (Chrysophanic acid)種天

3、然蒽醌，抑制EGF-誘導的 EGFR 磷酸化，且抑制 AKT 和mTOR/p70S6K 激活。IC50 & Target EGFR1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Chrysophanol (Chrysophanic Acid) blocks proliferation of colon cancer cells by inhibiting EGFR/mTORpathway. Chrysophanol, a natural anthraquinone, has anticancer activity in EGFR-ov

4、erexpressing SNU-C5human colon cancer cells. Chrysophanol treatment in SNU-C5 cells inhibits EGF-induced phosphorylation ofEGFR and suppresses activation of downstream signaling molecules, such as AKT, extracellular signal-regulated kinase (ERK) and the mammalian target of Rapamycin (mTOR)/ribosomal

5、 protein S6 kinase(p70S6K). Chrysophanol (80 and 120 M) significantly blocks cell proliferation when combined with themTOR inhibitor, Rapamycin. Chrysophanol inhibits EGF-induced phosphorylation of EGFR and suppressesactivation of AKT and mTOR/p70S6K, and significantly blocks cell proliferation. Chr

6、ysophanol dosedependently decreases CCK-8 and the viability of EGFR-overexpressing SNU-C5 cells. Chrysophanoltreatment dose-dependently decreases EGF induced phosphorylation of EGFR at Tyr1068. Chrysophanol(80 and 120 M) reduces the phosphorylation levels of mTOR at Ser2448. Chrysophanol (80 and 120

7、 M)also decreases the phosphorylation levels of p70S6K at Thr389. Chrysophanol inhibits EGF-induced EGFRactivation and suppresses activation of the downstream signaling molecules, AKT and mTOR/p70S6K 1.Chrysophanol (CA) inhibits lipid accumulation in 3T3-L1 adipocytes. Chrysophanol down-regulatesadi

8、pogenic factors in 3T3-L1 adipocytes. Chrysophanol induces thermogenic factors in primary culturedbrown adipocytes. Chrysophanol suppresses adipogenesis and induces thermogenesis via activation ofAMPK pathway 2.體內(nèi)研究 Chrysophanol (CA) improves HFD-induced obesity in C57BL/6 Mice. The in vivo performa

9、nce ofChrysophanol is performed in male C57BL/6J mice to determine the efficacy of administered Chrysophanol.Mice fed the HFD gained significantly more weight than those fed the standard diet mice. On the other hand,weight gain of Chrysophanol group is significantly less than with the untreated HFD.

10、 Mice in the HFD-groupgained 23.92 1.74 g of weight, while those in the Chrysophanol group gained 16.722 g of weight after 16weeks 2.PROTOCOLCell Assay 1 The cells are seeded at 5103 cells/mL in 96-well microplates and allowed to attach for 24 h. Chrysophanol(20, 50, 80 and 120 M) is added to the me

11、dium at various concentrations up to 120 M and for differentdurations. After treatment, cell cytotoxicity and/or proliferation is assessed by a Cell Counting Kit-8 (CCK-8).Briefly, highly water-soluble tetrazolium salt, WST-8, produces an orange colored water-soluble product,formazan. The amount of

12、formazan dye generated by dehydrogenases in cells is directly proportional to thenumber of living cells.CCK-8 (10 L) is added to each well and incubated for 3 h at 37C, then cellproliferation and cytotoxicity are assessed by measuring the absorbance at 450 nm using a microplatereader.Three replicate

13、d wells are used for each experimental condition 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administration 2 Male 4-week-old C57BL/6J mice are maintained for 1 week prior to experiments. Mice are maintained on a12-h light/dark cycle

14、in a pathogen-free animal facility, provided with laboratory diet and water ad libitum. Toinduce obesity, the mice are fed a HFD with 60% kcal% fat. Control group (C) are fed a commercial standardchow diet. HFD group (HFD) mice are fed with HFD only. HFD plus CA group (CA) Mice are fed with HFD for4

15、 weeks before administration of Chrysophanol (5 mg/kg/day). The mice are divided into three groups (n = 5)2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEthat are fed chow diet, HFD, and HFD plus Chrysophanol for 16 weeks. Body weight and food intake aremeasured three times per week.MCE has not ind

16、ependently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Acta Pharm Sin B. 2019 Jul; 9(4): 782793.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lee MS, et al. Chrysophanic acid blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway. Phytother Res. 2011Jun;25(6):833-7.2. Lim H, et al. Chrysophanic Acid Suppresses Adipogenesis and Induces Thermogenesis by Activating AMP-Activated Protein KinaseAlpha In viv