Parbendazole-SKF-29044-DataSheet-生命科學(xué)試劑-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作靶點(diǎn): Microtubule/Tubulin; Microtubule/Tubulin作通路: Cell Cycle/DNA Damage; Cytoskeleton儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mont

2、hs-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) 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. 請(qǐng)依序添加每種溶劑： 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 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 0.4 mg/mL (1.62 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Parbendazole種有效的 microtubule 重 組抑制劑，能夠破壞微管蛋，EC50 值為 8.79 nM，具有譜的驅(qū)作。IC50 & Target EC50: 8.79nM (tubulin) 1體外研究 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 您邊的抑制劑師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