A-484954 - CaMK 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEA-484954Cat. No.: HY-110096CAS No.: 142557-61-7分式: CHNO分量: 289.29作靶點(diǎn): CaMK作通路: Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 20 mg/mL (69.13 mM; Need ultrasonic)H2O : 90

2、% corn oilSolubility: 2 mg/mL (6.91 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 A-484954真核延長(zhǎng)因 2 (eEF2) 的度選擇性抑制劑，其 IC50 值為 280 nM。IC50 & Target IC50: 280 nM (eEF2) 1.體外研究 A-484954 is a highly selective eEF2K inhibitor with an IC50 value of 280 nM against

3、 eEF2K in the enzymaticassay and little activity against a wide panel of serine/threonine and tyrosine kinases. In enzymatic assay, theIC50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasingconcentrations of calmodulin 1.體內(nèi)研究 A484954 causes relaxation i

4、n E (+) and E (-) aorta or mesenteric artery precontracted with NA. Pretreatmentwith L-NAME but not indomethacin or cimetidine partially inhibits the A484954-induced relaxation inmesenteric artery 2. Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. It isrevealed that A-484954

5、 inhibits MCT-induced PA hypertrophy and fibrosis but not impairment of endothelium-dependent and -independent relaxation. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1expression and ROS generation as well as matrix metalloproteinase-2 activation 3.REFERENCES1. Chen Z, et al. 1-Benzyl-3

6、-cetyl-2-methylimidazolium iodide (NH125) induces phosphorylation of eukaryotic elongation factor-2 (eEF2): acautionary note on the anticancer mechanism of an eEF2 kinase inhibitor. J Biol Chem. 2011 Dec 23;286(51):43951-8.2. Kodama T, et al. Mechanisms underlying the relaxation by A484954, a eukary

7、otic elongation factor 2 kinase inhibitor, in rat isolatedmesenteric artery. J Pharmacol Sci. 2018 May;137(1):86-92.3. Kameshima S, et al. Eukaryotic elongation factor 2 kinase mediates monocrotaline-induced pulmonary arterial hypertension via reactiveoxygen species-dependent vascular remodeling. Am J Physiol Heart Circ Physiol. 2015 May 15;308(10):H1298-305.McePdfHeightCaution: Product has not been fully validated for medical applications.For researc