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Siramesine

Catalog No. T4620   CAS 147817-50-3
Synonyms: Lu 28-179

Siramesine (Lu 28-179)(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

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Siramesine Chemical Structure
Siramesine, CAS 147817-50-3
Pack Size Availability Price/USD Quantity
5 mg 4-6 weeks $ 207.00
10 mg 4-6 weeks $ 314.00
25 mg 4-6 weeks $ 479.00
50 mg 4-6 weeks $ 738.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Siramesine (Lu 28-179)(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
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.
Synonyms Lu 28-179
Molecular Weight 454.58
Formula C30H31FN2O
CAS No. 147817-50-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Cesen MH, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013 Oct 3;4:e818. 2. 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. 3. Spirkoski J, et al. Mast cell apoptosis induced by siramesine, a sigma-2 receptor agonist. Biochem Pharmacol. 2012 Dec 15;84(12):1671-80.

TargetMolCitations

1. Li Y, Xie X, Liao S, et al. A011, a novel small-molecule ligand of σ2 receptor, potently suppresses breast cancer progression via endoplasmic reticulum stress and autophagy. Biomedicine & Pharmacotherapy. 2022, 152: 113232

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Keywords

Siramesine 147817-50-3 GPCR/G Protein Sigma receptor Inhibitor lysosomes inhibit death cathepsin Sigma Receptor mitochondria selectivity Lu 28-179 cancer inhibitor

 

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