Siramesine

Description: Formerly known as Lu-28-179, siramesine is a potent and selective agonist of sigma-2 receptor agonist. Siramesine is able to trigger cancer cell death through destabilisation of mitochondria and exhibit promising anticancer activity in vivo. 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.

References: Cell Death Dis. 2013 Oct 3; 4:e818.

Related CAS#: 224177-60-0 (HCl); 163630-79-3 (fumarate)