Siramesine_147817-50-3_DataSheet_MedChemExpress

Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :Siramesine147817-50-3HY-14221454.58C30H31FN2O>98%Solubility:DMSOMechanisms: Pathways:GPCR/G protein; Target:Sigma Receptor Biological Activity:Siramesine, a sigma2 receptor agonist siramesine has been shown to trigger cell death of cancerSiramesineasigma-2receptoragonistsiramesinehasbeenshowntotriggercelldeathofcancercells and to exhibit a potent anticancer activity in vivo. IC50 value: Target: sigma-2 receptor; lysosome-destabilizing agent siramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. InHaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrialmembrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptoticmorphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMPwas rapidly lost [1]. Siramesine, a sigma-2 receptor agonist originally developed as an anti-depressant, can induce cell death in transformed cells through a mechanism involving lysosomaldestabilization [2]. in vivo: SA4503 or siramesine given jointly with MEM (as well as with...References:[1]. ?esen MH, et al. Siramesine triggers cell death through destabilisation of mitochondria, but notlysosomes. Cell Death Dis. 2013 Oct 3;4:e818. [2].SpirkoskiJ,etal.Mastcellapoptosisinducedbysiramesine,asigma-2[2]. Spirkoski J, et al. Mast cell apoptosis induced by siramesine, a sigma2 receptor agonist.receptoragonist.Biochem Pharmacol. 2012 Dec 15;84(12):1671-80. [3]. Skuza G, et al. The synergistic effect of selective sigma receptor agonists and uncompetitiveNMDA receptor antagonists in the forced swim test in rats. J Physiol Pharmacol. 2006Jun;57(2):217-29. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 08540,USAEmail: info@medchemexpress.com Web: www.medchemexpress.com