"目錄號: HY-14221
Siramesine(Lu 28-179)是sigma-2受體激動劑，能引發(fā)癌細胞的死亡，并在體內具有抗癌活性。
相關產品
UNC0642-SA4503 dihydrochloride-Dextromethorphan hydrobromide hydrate-Noscapine-PRE-084 hydrochloride-S1RA hydrochloride-4-IBP-BD-1047 dihydrobromide-Siramesine hydrochloride-BD1063 dhydrochloride-Anavex 2-73-CYR-101-Dimemorfan phosphate-Sigma-LIGAND-1-
生物活性
Description
Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. IC50 value:Target: sigma-2 receptor; lysosome-destabilizing agentsiramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. In HaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrial membrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptotic morphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMP was 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 lysosomal destabilization [2].in vivo: SA4503 or siramesine given jointly with MEM (as well as with AMA) decreased the immobility time in rats. The effect of SA4503 and AMA co-administration was antagonized by progesterone, a sigma1 receptor antagonistic neurosteroid. Combined treatment with siramesine and AMA was modified by neither progesterone nor BD1047 (a novel sigma antagonist with preferential affinity for sigma1 sites) [3]
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