Siramesine
Based on 6 publication(s) in Google Scholar
Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity.
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- Purity: 98.98%
- CAS No.: 147817-50-3
- 화학식: C30H31FN2O
- 분자량:454.58
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보관:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) Siramesine
MoreAll Sigma Receptor Isoforms
More
Biological Activity
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Sigma 1 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C6 | EC50 |
43.1 μM
Compound: Lu-28-179
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Antiproliferative activity against rat C6 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Antiproliferative activity against rat C6 cells assessed as reduction in cell viability after 24 hrs by MTT assay
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10.1039/C5MD00079C |
| DU-145 | EC50 |
13.9 μM
Compound: Lu-28-179
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Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 24 hrs by MTT assay
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10.1039/C5MD00079C |
| EMT6 | EC50 |
14.9 μM
Compound: 6
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Antagonist activity at sigma-2 receptor in mouse EMT6 cells assessed as inhibition of cell proliferation after 24 hrs by MTS assay
Antagonist activity at sigma-2 receptor in mouse EMT6 cells assessed as inhibition of cell proliferation after 24 hrs by MTS assay
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[PMID: 24821398] |
| EMT6 | EC50 |
5.3 μM
Compound: 6
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Antagonist activity at sigma-2 receptor in mouse EMT6 cells assessed as inhibition of cell proliferation after 48 hrs by MTS assay
Antagonist activity at sigma-2 receptor in mouse EMT6 cells assessed as inhibition of cell proliferation after 48 hrs by MTS assay
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[PMID: 24821398] |
| MCF7 | EC50 |
12.3 μM
Compound: Lu-28-179
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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10.1039/C5MD00079C |
| MCF7 | EC50 |
23.6 μM
Compound: Lu-28-179
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay
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10.1039/C5MD00079C |
| MCF7 | IC50 |
13 μM
Compound: Srms
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Cytotoxicity against ER/PR-positive HER2-negative human MCF7 cells harbouring p53 R175H mutant assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
Cytotoxicity against ER/PR-positive HER2-negative human MCF7 cells harbouring p53 R175H mutant assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
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[PMID: 35724925] |
| SK-BR-3 | IC50 |
14 μM
Compound: Srms
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Cytotoxicity against ER/PR-negative HER2-positive human SK-BR-3 cells harbouring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
Cytotoxicity against ER/PR-negative HER2-positive human SK-BR-3 cells harbouring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based assay
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[PMID: 35724925] |
Siramesine displays the binding affinities: IC50 (sigma 1)=17 nM, IC50 (sigma 2)=0.12 nM, IC50 (5-HT1A)=21000 nM, IC50 (5-HT1A)=2000 nM, IC50 (D2)=800 nM, IC50 (alpha 1)=330 nM[1].
Siramesine (0-50μM; 8 hours) induces cell death in various cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y and glioblastoma cell line U-87MG)[2].
Siramesine (0-40 μM; 2-48 hours) activates caspases in HaCaT and in U-87MG cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 147817-50-3
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Appearance Oil
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분자량 454.58
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화학식 C30H31FN2O
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Color Colorless to light yellow
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SMILES
FC1=CC=C(N2C=C(CCCCN3CCC4(CC3)OCC5=C4C=CC=C5)C6=C2C=CC=C6)C=C1
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Synonyms
Lu 28-179
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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J Am Chem Soc
Fluorinated Ribonucleocarbohydrate Nanoparticles Allow Ultraefficient mRNA Delivery and Protein Expression in Tumor-Associated Myeloid Cells. [Abstract]2025 Mar 26. PMID: 40135499 -
Adv Sci (Weinh)
2023 May;10(13):e2300311. PMID: 36905240 -
Sci Adv
Quantitative prediction of siRNA complexation by ionizable drugs enables their codelivery in nanoparticles. [Abstract]2026 Jun 12;12(24):eaed2731. PMID: 42284421 -
J Pharmacol Exp Ther
Characterization of CM572, a Selective Irreversible Partial Agonist of the Sigma-2 Receptor with Antitumor Activity. [Abstract]2015 Aug;354(2):203-12. PMID: 26034081 -
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순도&문서
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Perregaard J, et al. Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. J Med Chem. 1995;38(11):1998-2008. [Content Brief]
[2]. Česen MH, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013;4(10):e818. Published 2013 Oct 3. [Content Brief]
[3]. Ostenfeld MS, et al. Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Autophagy. 2008;4(4):487-499. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Siramesine Related Classifications
HY-14221 Related Classifications
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