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Siramesine hydrochloride

Chemical Structure : Siramesine hydrochloride

CAS No.: 224177-60-0

Siramesine hydrochloride (Lu 28-179, Lu28-179)

Catalog No.: PC-28289Not For Human Use, Lab Use Only.

Siramesine hydrochloride (Lu 28-179) is a lysosomotropic agent and potent, selective sigma-2 receptor ligand and agonist with binding IC50 of 0.12 nM, exhibits 140-fold selectivity over Sigma-1 receptor.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Siramesine hydrochloride (Lu 28-179) is a lysosomotropic agent and potent, selective sigma-2 receptor ligand and agonist with binding IC50 of 0.12 nM, exhibits 140-fold selectivity over Sigma-1 receptor.
Siramesine inhibits acid sphingomyelinase (ASM) by interfering with the binding of ASM to its essential lysosomal cofactor, bis(monoacylglycero)phosphate.
Siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation.
Siramesine induces lysosomal leakage and cathepsin-dependent death of cancer cells in vitro and displays potent anti-cancer activity in vivo.
Siramesine effectively induces caspase-independent programmed cell death in immortalized and transformed cells of various origins.

Physicochemical Properties

M.Wt 491.05
Formula C30H32ClFN2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1'-(4-(1-(4-Fluorophenyl)-1H-indol-3-yl)butyl)-3H-spiro[isobenzofuran-1,4'-piperidine] hydrochloride

References

1. Česen MH, et al. Cell Death Dis. 2013 Oct 3;4(10):e818.

2. Petersen NH, et al. Cancer Cell. 2013 Sep 9;24(3):379-93.

3. Zeng C, et al. Br J Cancer. 2012 Feb 14;106(4):693-701.

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