Hispidulin-Dinatin-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHispidulinCat. No.: HY-N1950CAS No.: 1447-88-7Synonyms: Dinatin分式: CHO分量: 300.26作靶点: Pim作通路: JAK/STAT Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 62.5 mg/mL (208.15 mM; Need ul

2、trasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (6.93 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (6.93 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL

3、(6.93 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Hispidulin具有泛物活性的天然黄酮。 Hispidulin是Pim-1的抑制剂，IC50值为2.71 M。IC50 & Target IC50: 2.71 M (Pim-1) 1体外研究 Hispidulin induces cell death in a dose- and time-dependent manner in HepG2 cells. Hispidulin inducesapoptosis through mitochondrial dysfunction, which is

4、 characterized by decreased Bcl-2/Bax ratio, disruptedmitochondrial membrane potential and increased release of cytochrome C and activated capase-3 2.体内研究 Hispidulin shows significant inhibitory effect on mice tumor size 2. Hispidulin treatment effectively preventsovariectomy-induced body weight los

5、s and attenuates ovariectomy-induced bone loss. Hispidulin treatmentalso decreases trabecular spacing in ovariectomy mice 3. Intraperitoneally administering hispidulin(10 or50mg/ kg) to rats 30 min before intraperitoneally injecting kainic acid (15mg/kg) increases seizure latencyand decreases seizur

6、e score. In addition, hispidulin substantially attenuates kainic acid-induced hippocampalneuronal cell death, and this protective effect is accompanied by the suppression of microglial activation andthe production of proinflammatory cytokines such as interleukin-1, interleukin-6, and tumor necrosis

7、factor-in the hippocampus 4.PROTOCOLCell Assay 2 HepG2 cells are treated with different concentrations of hispidulin (50, 100, 200 M) for 24, 48 and 72 h.Following treatment, cells are further incubated with MTT reagents at 37C for 4 h before DMSO is added, todissolve farmazan crystals, and absorban

8、ce is measured at 570 nm in a microplate reader 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Tumor are established in mice. Mice are treated with DMSO or Hispidulin at a dosage of 10, 20 or 40Administration 2 mg/kg/day for 35 days. The

9、 body weight of tumour-bearing mice is recorded every week and tumour volumeis calculated 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chao SW, et al. Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-o

10、ncogene KinasePim-1. J Nat Prod. 2015Aug 28;78(8):1969-76.2. Gao H, et al. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2cancer cells. Cell Biochem Biophys. 2014 May;69(1):27-34.3. Zhou R, et al. Hispidulin exerts anti-osteoporot

11、ic activity in ovariectomized mice via activating AMPK signaling pathway. Cell BiochemBiophys. 2014 Jun;69(2):311-7.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE4. Lin TY, et al. Protective effect of hispidulin on kainic acid-induced seizures and neurotoxicity in rats. Eur J Pharmacol. 2015 May15;755:6-15.McePdfHeightCaution: Product has not