Go-6983-G-6983-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGo 6983Cat. No.: HY-13689CAS No.: 133053-19-7Synonyms: G 6983; Goe 6983分式: CHNO分量: 442.51作靶点: PKC作通路: Epigenetics; TGF-beta/Smad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 DMSO : 34 mg/mL (76.

2、83 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.65 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.65 mM); Suspended solution; Need ultrasonic3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubil

3、ity: 2.5 mg/mL (5.65 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY物活性 Go 6983种有效的 PKC 抑制剂，能够作于 PKC，PKC，PKC，PKC 和 PKC，IC50 值分别为 7nM，7 nM，6 nM，10 nM 和 60 nM。IC50 & Target PKC PKC PKC PKC6 nM (IC50) 7 nM (IC50) 7 nM (IC50) 10 nM (IC50)PKC PKC60 nM (IC50) 20000 nM (IC50)体外研究 Go 6983 inhibi

4、ts PKC with IC50 of 20 M, and the pther PKC isoenzymes can be suppressed by Go 6983with IC50 values from 7 to 60 nM 1. Go 6983 (100 nM) significantly reduces PMN adherence to theendothelium and infiltration into the myocardium compared with I/R + PMN hearts, and significantly inhibitssuperoxide rele

5、ase from PMNs by 90 +/- 2% in rat hearts 2. Go 6983 (200 nM) has a reducedcardioprotective effect compared with the cardioprotective Go 6983 concentrations (50 and 100 nM) despiteinhibiting PMN superoxide release by 99% 3.PROTOCOLKinase Assay 1 Phosphorylation reactions are carried out in a total vo

6、lume of 100 L, containing buffer C (50 mM Tris-HCl,pH 7.5, 10 mM -mercaptoethanol), 4 mM MgCl2, 10 g PS, 100 nM TPA, 5 L of a Sf158 cell extract as asource of recombinant PKC or of Sf9 cell extracts as a source of other recombinant PKC isoenzymes, 10 gof syntide 2 as substrate, and 35 M ATP containi

7、ng 1 Ci -32PATP. In some experiments, PS and TPAare omitted or various inhibitors at concentrations indicated in the text are added. After incubation for 10 minat 30C, the reaction is terminated by transferring 50 L of the assay mixture onto a 20 mm square piece ofphosphocellulose paper, which is wa

8、shed 3 times in deionized water and twice in acetone. The radioactivityon each paper is determined by liquid scintillation counting.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 Cell Death Dis. 2018 Feb 7;9(2):165. Sci Rep. 2017 Oct 19;7(1

9、):13571. J Appl Toxicol. 2016 Nov;36(11):1409-17. Vet Microbiol. 2016 Aug 30;192:26-33. Biochem Biophys Res Commun. 2018 Sep 3;503(1):62-70.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemESee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Gschwendt M, et al. Inhibition of protein

10、 kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett,1996, 392(2), 77-80.2. Peterman EE, et al. G0 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion. J Cardiovasc Pharmacol, 2004, 43(5),645-656.3. Young LH, et al. G0 6983: a fast acting protein kinase C inhibitor that attenuates myocardial ischemia/reperfusion injury. CardiovascDrug Rev, 2005, 23(3), 255-272.McePdfHeightCaution: Product has not been full