Iberin-NSC-321801-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIberinCat. No.: HY-101413CAS No.: 505-44-2Synonyms: NSC 321801分式: CHNOS分量: 163.26作靶点: Apoptosis; Endogenous Metabolite作通路: Apoptosis; Metabolic Enzyme/Protease储存式: Pure form -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 m

2、onth溶解性数据体外实验 DMSO : 310 mg/mL (1898.81 mM)Ethanol : 10 mg/mL (61.25 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 6.1252 mL 30.6260 mL 61.2520 mL5 mM 1.2250 mL 6.1252 mL 12.2504 mL10 mM 0.6125 mL 3.0626 mL 6.1252 mL请根据产品在不同溶剂中的溶解度，选择合

3、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: 2.5 mg/mL (15.31 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in sa

4、line)1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (15.31 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (15.31 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Iberin萝硫素的亚砜类似物，是天然存在的异硫氰酸酯家族的成员。抑制HL60细胞的IC50值为2.3 M。IC50 & Target Human Endogenous Metabol

5、ite体外研究 Iberin inhibits the growth of neuroblastoma cells in a dose- and time-dependent manner. The iberin-inducedcell cycle arrest in neuroblastoma cells is associated with inhibition of expression of cyclin-dependent kinaseCdk2, Cdk4, and Cdk6 proteins. There is an increase in apoptotic cell death

6、 in iberin treated cells ascompared with control cells. The iberin-induced apoptosis is found to be associated with activation ofcaspase-9, caspase-3, and PARP 2. Iberin inhibits growth of human glioblastoma cells in cell proliferationassays, enhances cytotoxicity, and induces apoptosis by activatio

7、n of caspase-3 and caspase-9 3.体内研究 Iberin is tested in an in vivo foreign-body infection mouse model, and the results show no significantlydifference in bacterial clearance between treated and nontreated miced 4. Iberin increases tissue levels ofthe phase II detoxification enzymes quinone reductase

8、 and glutathione S-transferase in a variety of rattissues 5.PROTOCOLCell Assay 2 Cells are plated at a density of 1105 cells/well in microtiter plates and treated with different concentrationsof iberin (1, 2.5, 10 and 25 M). Then 20 L of 5 mg/mL MTT in PBS, is added to each well and allowed toincuba

9、te for a further 4 h. After 4 h of incubation, 100 L of DMSO is added to each well to dissolve theformazan crystals. Absorbance values at 550 nm are measured with a microplate reader 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: Groups

10、of five rats are dosed by oral intubation with the test compounds, as solutions in soybean oil,Administration 45 each day for 5 days. This doses used are 4.0 mg/kg/day for AITC, 5.9 mg/kg/day for iberverin, 6.5 mg/kg/dayfor iberin, 6.4 mg/kg/day for erucin, 7.1 mg/kg/day for sulforaphane, and 7.2 mg

11、/kg/day for cheirolin. Thevolume of solution administered is 2 mL/kg in all cases. Ten control rats are dosed with soybean oil alone 5.Mice: Iberin is diluted in 96% ethanol to a concentration of 32 mg/mL followed by a 40 x dilution in 0.9% NaCl.The mice are injected with 0.2 mL of the final solutio

12、n, corresponding to 8 g/g of body weight. The placebogroup is injected with a 2.4% ethanol solution (96% ethanol0.9% NaCl) corresponding to the amount ofethanol that the iberin-treated group received. Mice are treated every 12 h from day 2 preinsertion to day 2postinsertion, and treatment is continu

13、ed until 12 h before the mice are euthanized 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Jakubikova J, et al. Isothiocyanates induce cell cycle arrest, apoptosis and mitochondrial poten

14、tial depolarization in HL-60 andmultidrug-resistant cell lines. Anticancer Res. 2005 Sep-Oct;25(5):3375-86.2. Jadhav U, et al. Iberin induces cell cycle arrest and apoptosis in human neuroblastoma cells.3. Jadhav U, et al. Dietary isothiocyanate iberin inhibits growth and induces apoptosis in human

15、glioblastoma cells. J Pharmacol Sci. 2007Feb;103(2):247-51.4. Jakobsen TH, et al. Food as a source for quorum sensing inhibitors: iberin from horseradish revealed as a quorumsensing inhibitor ofPseudomonas aeruginosa. Appl Environ Microbiol. 2012 Apr;78(7):2410-21.5. Munday R, et al. Induction of phase II detoxification enzymes in rats by plant-derived isothiocyanates: comparison of allyl isothiocyanatewith sulforaphane and related compounds. J Agric Foo