TargetMol

Siramesine

Product Code:
 
TAR-T4620
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T4620-5mg5mg£237.00
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TAR-T4620-10mg10mg£323.00
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TAR-T4620-25mg25mg£455.00
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TAR-T4620-50mg50mg£663.00
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Further Information

Bioactivity:
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.lysosome-destabilizing agent siramesine 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
CAS:
147817-50-3
Formula:
C30H31FN2O
Molecular Weight:
454.589
Pathway:
GPCR/G Protein
Purity:
0.98
SMILES:
Fc1ccc(cc1)-n1cc(CCCCN2CCC3(CC2)OCc2ccccc32)c2ccccc12
Target:
Sigma receptor

References

Li Y, Xie X, Liao S, et al. A011, a novel small-molecule ligand of ?2 receptor, potently suppresses breast cancer progression via endoplasmic reticulum stress and autophagy. Biomedicine & Pharmacotherapy. 2022, 152: 113232 Cesen MH, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013 Oct 3;4:e818. Skuza G, et al. The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats. J Physiol Pharmacol. 2006 Jun;57(2):217-29. Spirkoski J, et al. Mast cell apoptosis induced by siramesine, a sigma-2 receptor agonist. Biochem Pharmacol. 2012 Dec 15;84(12):1671-80.