Nifurtimox - Parasite 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENifurtimoxCat. No.: HY-W040073CAS No.: 23256-30-6分式: CHNOS分量: 287.3作靶点: Parasite; Lactate Dehydrogenase作通路: Anti-infection; Metabolic Enzyme/Protease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

2、 DMSO : 150 mg/mL (522.10 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.70 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 Nifurtimox种于治疗锥病 (Trypanosoma cruzi) 的抗剂。Nifurtimox 可于治疗神经母细胞瘤细胞。Nifurtimox影响乳酸脱氢酶 (LDH) 活性。IC50

3、 & Target Trypanosoma cruzi 1Lactate dehydrogenase (LDH) 1体外研究 Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH). To differentiate if this effect is a result of areduced LDH activity or a shift in pyruvate metabolism due to activation of PDH, the enzyme activity of LDH isdetermined a

4、fter 4 h treatment with 50 g/mL Nifurtimox. Compared to the untreated control, the LDH activityis significantly reduced for LA-N-1 (P=0.005), IMR-32 (P=0.009), LS (P=0.0035) and SK-N-SH (P=0.0065).Nifurtimox reduces cell viability and induces cell cycle arrest and apoptosis in neuroblastoma cells. T

5、ocharacterize the cytotoxic impacts of Nifurtimox on neuroblastoma, 4 cell lines are subjected to severalexperiments. Cell viability is reduced for all 4 neuroblastoma cell lines after 24 h incubation with 50 g/mL toan average of 66%, 63%, 62% and 75% (LA-N-1, IMR-32 LS and SK-N-SH, respectively). T

6、he reduction issignificant compared to the untreated control (P 1.PROTOCOLCell Assay 1 The Neuroblastoma cell lines IMR-32, LA-N-1 and SK-N-SH and the neuroblastoma cell line LS are grown inRPMI-1640 medium supplemented with 10% (v/v) fetal calf serum (FCS), 2 mM L-glutamine, 100 U/mLPenicillin and

7、100 g/mL Streptomycin and incubated at 37C, 5% CO2 and saturated humidity. To assessthe cell viability after incubation with Nifurtimox at different concentrations (10 g/mL up to 50 g/mL or 34.8M to 174 M, respectively in the supernatant growth medium) or the vehicle control with accordingconcentrat

8、ions, all neuroblastoma cell lines are subjected to an MTS assay. Stock solutions of MTS aremade at 480 M in sterile filtered deionized water and stored at -20C. Cells are grown to approximately 50%confluency, treated with Nifurtimox, and incubated for 1 h with fresh media containing 12 M MTS 1.MCE

9、has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Cabanillas Stanchi KM, et al. Nifurtimox reduces N-Myc expression and aerobic glycolysis in neuroblastoma. Cancer Biol Ther.2015;16(9):1353-63.McePdfHeightCaution: Product has not been fully validated for medical