Parbendazole-SKF-29044-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEParbendazoleCat. No.: HY-115364CAS No.: 14255-87-9Synonyms: SKF 29044分式: CHNO分量: 247.29作靶点: Microtubule/Tubulin; Microtubule/Tubulin作通路: Cell Cycle/DNA Damage; Cytoskeleton储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mont

2、hs-20C 1 month溶解性数据体外实验 DMSO : 4 mg/mL (16.18 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 0.4 mg/mL (1.62 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.4 mg/mL (1.62 mM); Suspended solution; Need ultrasonic1/3 Master

3、 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: 0.4 mg/mL (1.62 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Parbendazole种有效的 microtubule 重 组抑制剂，能够破坏微管蛋，EC50 值为 8.79 nM，具有谱的驱作。IC50 & Target EC50: 8.79nM (tubulin) 1体外研究 Parbendazole is a tubulin destabilizer, with a

4、n EC50 of 8.79nM, and can induce DNA damage 1.Parbendazole (2-10 M) inhibits the assembly of microtubules dose-dependently, with an IC50 of 3 M.Parbendazole (2-20 M)-treated cells show an complete absence of microtubules in Vero cells 2.Parbendazole (up to 10 M) inhibits the growth of CLd-AXE myxamo

5、ebae. Parbendazole (2-5 M) potentlyinhibits tubulin purified from the wild-type myxamoebae 3.PROTOCOLKinase Assay 2 Pure tubulin is obtained from sheep brain by 2 cycles of assembly and disassembly in vitro. Immediately priorto use the protein is centrifuged at 130000 g for 30 min to remove any aggr

6、egates. It is used at a proteinconcentration of 0-2 mg/mL in 0.025 M Pipes buffer, 0-5 mM EGTA, 0-25 mM Mg2SOsup4, 0.1 mM GTP.Drug binding is determined by equilibrium dialysis using concentrations of parbendazole between 0.1 M and4 M, and 2% (v/v) DMF (dimethyl formamide) as a carrier. Equilibrium

7、is achieved by constant stirring for 2h at 26C, bovine serum albumin being used as a standard. 200 L aliquots are counted in PCS in a 25-200Bliquid scintillation counter 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 Vero cells, an estab

8、lished cell line derived from monkey kidney are seeded in DMEM supplemented with10% (v/v) foetal calf serum onto glass coverslips in multiwell dishes. They are allowed to settle, and spreadfor 2-5 h in a humid atmosphere at 37C. After this time the medium is changed to DMEM containing 2, 10 or20 M p

9、arbendazole and 1% (v/v) DMSO controls contained 1 % (v/v) DMSO or had no additions 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Lo YC, et al. Computational Cell Cycle Profiling of Cancer Cells for Prioritizing FDA-Approved Drugs with

10、Repurposing Potential. SciRep. 2017 Sep 12;7(1):11261.2. Lo YC, et al. Computational Cell Cycle Profiling of Cancer Cells for Prioritizing FDA-Approved Drugs with Repurposing Potential. SciRep. 2017 Sep 12;7(1):11261.3. Havercroft JC, et al. Binding of parbendazole to tubulin and its influence on mi

11、crotubules in tissue-culture cells as revealed byimmunofluorescence microscopy. J Cell Sci. 1981 Jun;49:195-204.4. Havercroft JC, et al. Binding of parbendazole to tubulin and its influence on microtubules in tissue-culture cells as revealed by2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEimmunof

12、luorescence microscopy. J Cell Sci. 1981 Jun;49:195-204.5. Foster KE, et al. A mutant beta-tubulin confers resistance to the action of benzimidazole-carbamate microtubule inhibitors both in vivoand in vitro. Eur J Biochem. 1987 Mar 16;163(3):449-55.6. Foster KE, et al. A mutant beta-tubulin confers resistance to the action of benzimidazole-carbamate microtubule inhibitors both in vivoand in vitro. Eur J Biochem. 1987 Mar 16;163(3):449-55.McePdfHeightCau