Piperlongumine-Piplartine-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPiperlongumineCat. No.: HY-N2329CAS No.: 20069-09-4Synonyms: Piplartine分式: CHNO分量: 317.34作靶点: ERK; Reactive Oxygen Species; Autophagy; Apoptosis作通路: MAPK/ERK Pathway; Stem Cell/Wnt; Immunology/Inflammation; Metabolic Enzyme/Prot

2、ease; NF- B; Autophagy; Apoptosis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 : 125 mg/mL (393.90 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1512 mL 15.7560 mL 31.5119 mL5 mM 0.6302 mL 3.1512 mL 6.3024 mL10 mM 0.3151 mL 1.5756 mL

3、3.1512 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (6.55 mM); Clear solution2. 请依序添加每种溶剂： 10

4、% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (6.55 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (6.55 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Piperlongumine从荜茇中得到的物碱 1，具有抗炎、抗 、抗管成、抗氧化、抗肿瘤和抗糖尿病等活性 2。在肿瘤细胞中，P

5、iperlongumine 能够诱导 ROS 和凋亡 1。Piperlongumine 具有抗肌纤维化的作，通过抑制 ERK1/2 信号通路抑制肌成纤维细胞的转化 2。IC50 & Target ERK1 ERK2体外研究 Piplartine (5, 10, and 15 M) significantly decreases cell proliferation of 786-O, SKBR3, Panc1, A549, andL3.6pL cancer cells after treatment for 24 and 48 hours, induces apoptosis and ROS

6、in these cell lines at 5and 10 M after 3 or 9 h of treatment 1.Piplartine (5 or 10 M) induces cleaved PARP and downregulates Sp1, Sp3, Sp4, and Sp-regulated genes1.Piplartine (20 M) decreases the viability of cardiac fibroblasts (CFs). Piplartine (0-10 M) suppressesmyofibroblast transformation via s

7、uppression of the ERK1/2 signaling pathway 2.体内研究 Piperlongumine (30 mg/kg/day, i.p. for 3 weeks) exhibits potent anti-tumor effect in athymic nude micebearing L3.6pL cells without body weight loss 1.REFERENCES1. Karki K, et al. Piperlongumine Induces Reactive Oxygen Species (ROS)-Dependent Downregu

8、lation of Specificity Protein TranscriptionFactors.2. Wu X, e,t al. Piperlongumine inhibits angiotensin II-induced extracellular matrix expression in cardiac fibroblasts. J Cell Biochem. 2018Dec;119(12):10358-10364McePdfHeightCaution: Product has not been fully validated for medical applications.For