5-Iodotubercidin-NSC-113939-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE5-IodotubercidinCat. No.: HY-15424CAS No.: 24386-93-4Synonyms: NSC 113939; 5-ITu分式: CHINO分量: 392.15作靶点: Adenosine Kinase作通路: Metabolic Enzyme/Protease; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months

2、-20C 1 month溶解性数据体外实验 DMSO : 49 mg/mL (124.95 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5500 mL 12.7502 mL 25.5004 mL5 mM 0.5100 mL 2.5500 mL 5.1001 mL10 mM 0.2550 mL 1.2750 mL 2.5500 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 5-Iodotuber

3、cidin (5-ITU) is prepared fresh daily by dissolving in saline with 2% ethanol (v/v)5.BIOLOGICAL ACTIVITY物活性 5-Iodotubercidin种有效的腺苷激酶抑制剂，IC50 值为 26 nM。IC50 & Target IC50: 26 nM (adenosine kinase)1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 5-Iodotubercidin (40 M) enhances the rate of phospho

4、rylase inactivation and shortens the lag before theactivation of glycogen synthase. 5-Iodotubercidin (50 M) antagonizes the effects of glucagon andvasopressin, but does not affect the basal concentration of free calcium in single hepatocytes 1. 5-Iodotubercidin (20 M) causes an important decrease in

5、 ATP concentration, and a concomitant smallerincrease in AMP concentration. 5-Iodotubercidin decreases the activity of ACC and the rates of synthesis offatty acids and cholesterol. In line with the iodotubercidin-mediated inhibition of ACC, 5-iodotubercidininduces a marked decrease in the intracellu

6、lar concentration of malonyl-CoA 3. 5-Iodotubercidin causes astrong decrease in the immunofluorescence levels of P-T3-H3, and depletion of P-T3-H3 is complete at 10M 5-5-iodotubercidin 4.体内研究 5-Iodotubercidin (1 mL/kg, i.p.) is in agreement with activity observed against bicuculline-induced seizures

7、following local administration of the AKI into the prepiriform cortex 2.PROTOCOLKinase Assay 2 AK activity is measured in a radiochemical assay. The final reaction volume is 100 L and contained 70 mMTris-maleate (pH 7.0), 0.1% (w/v) bovine serum albumin, 1.0 mM MgCl2, 1.0 mM ATP, 1.0 M U-14Cadenosin

8、e (400-600 mCi/mmol) and various inhibitor concentrations. Inhibitors are prepared as 10 mMstock solutions in DMSO. The final DMSO concentration in the assay is 5% (v/v). Eleven differentconcentration of the test solutions ranging from 0.001 to 10.0 M are utilized to determine a dose responsecurve o

9、f the inhibition of the enzyme. Reactions are started by adding the appropriate amount of purifiedhuman recombinant AK and incubated for 20 min at 37C. The reactions are terminated by addition of thepotent AKI GP3269. A 30-L aliquot of each reaction is spotted on DEAE cellulose filter paper (cut in

10、squaresof appr 11 cm) and air-dried for 30 min. The dry filters are then washed for 3 min in deionized water toremove residual U-14Cadenosine, rinsed with ethanol and dried at 90C for 20 min. The filter papers arecounted in 5.5 mL of Ready Safe liquid scintillation cocktail using a Beckman LS3801 sc

11、intillation counter.Control AK activity is determined from the amount of 14CAMP formed in the presence of 5% DMSO. Theconcentration of inhibitor required to inhibit 50% of the AK activity (IC50) is determined graphically from plotsof inhibitor concentration versus percent (%) control enzyme activity

12、.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 4 HeLa cells are grown in DME supplemented with 10% fetal bovine serum (FBS) and 2 mM l-glutamine.Nocodazole is used at a concentration of 3.3 M unless differently specified. Thymidine (2.5 mM)

13、 is used inthe asssay. For transfection, FuGENE 6 Transfection Agent is used at a 3:1 ratio with plasmid DNA. Cells areanalyzed 24-48 h after transfection.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Male SA rats (100-150 g) are maintained on

14、a 12:12 light:dark cycle in temperaturecontrolled facilities withAdministration 2 free access to food and water. One hour prior to seizure testing, the animals are injected intraperitoneally (1mL/kg) with DMSO vehicle or with test compound dissolved in DMSO. At the time of the test, an electrolyteso

15、lution (2% lidocaine in 0.9% sodium chloride) is applied to the eyes. Maximal electroshock seizures areinduced by administering a 60-Hz current of 150 mA for 0.2 s via corneal electrodes, using a WahlquistModel H stimulator. The endpoint measured is suppression of hindlimb tonic extension (HTE) and

16、expressed2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEas percentage of animals in which the response is inhibited. At this supramaximal stimulation level, virtually100% of control (vehicle-treated) animals show HTE. ED50 values are calculated from a dose-responsecurve using probit analysis. The

17、N for the screening doses is 6-8; doseresponse determinations areconducted with at least 5 animals/dose.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Sci Rep. 2017 Feb 21;7:42885. Front Mol Neurosci. 2016 Jun 3;9:42. Acta Crystallogr F Str

18、uct Biol Commun. 2019 Jul 1;75(Pt 7):515-519.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Massillon D, et al. Identification of the glycogenic compound 5-iodotubercidin as a general protein kinase inhibitor. Biochem J. 1994 Apr1;299 (Pt 1):123-8.2. Ugarkar BG, et al. Adenosine kinase inhibitors. 1. Synthesis, enzyme inhibition, and antiseizure activity of 5-iodotubercidin analogues. JMed Chem. 2000 Jul 27;43(15):2883-93.3. Garca-Villafranca J, et al. Effects of 5-iodotubercidin on hepatic fatty