Salinomycin

SKU: orb1710669

Description

Salinomycin (Procoxacin) is a polyether ionophore antibiotic active against gram-positive bacteria. It potently inhibits the Wnt/β-catenin pathway by blocking LRP6 phosphorylation and selectively targets cancer stem cells, making it a valuable tool for oncology and stem cell research in both in vitro and in vivo models.

Research Area

Cell Biology, Infectious Disease & Virology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 53003-10-4
• MW: 751
• Purity: 98.00% (May vary between batches)
• Formula: C₄₂H₇₀O₁₁
• SMILES: [H][C@@]1(CC[C@H](C)[C@@]([H])(O1)[C@@H](C)[C@H](O)[C@H](C)C(=O)[C@H](CC)[C@@]1([H])O[C@@]2(O[C@@]3(CC[C@](C)(O3)[C@@]3([H])CC[C@](O)(CC)[C@H](C)O3)[C@H](O)C=C2)[C@H](C)C[C@@H]1C)[C@@H](CC)C(O)=O
• Target: Autophagy,Wnt/beta-catenin,Antibiotic,Antibacterial,Parasite,Mitophagy,Apoptosis
• Solubility: DMSO:140 mg/mL (186.42 mM)

Bioactivity

• In Vivo:
  Upon administering doses of 4 mg/kg and 8 mg/kg Salinomycin (Sal), alongside 10 uL/g saline water to mice for a duration of 6 weeks, followed by their sacrifice, a significant reduction in liver tumor size is observed in the Sal-treated groups compared to the controls. Tumor diameters decrease notably from 12.17 mm to 3.67 mm (p<0.05), and volumes, calculated as V=length×width^2×0.5, diminish from 819 mm^3 to 25.25 mm^3 (p<0.05). Subsequent analyses, involving HE staining, immunohistochemistry, and TUNEL assays, are conducted to evaluate Salinomycin's anti-tumor efficacy. Results show altered liver cancer tissue structure, reduced PCNA expression, and higher apoptosis rates in Sal-treated mice, indicating significant anti-tumor activity. Furthermore, an increase in the Bax/Bcl-2 ratio and a decrease in β-catenin protein expression corroborate Salinomycin's effectiveness. Salinomycin, a monocarboxylic acid polyether antibiotic derived from Streptomyces albus fermentation, exhibits a unique cyclic structure enabling it to bind with pathogenic microorganisms and extracellular cations of coccidia, particularly K+, Na+, Rb+, effectively altering intra- and extracellular ion concentrations.
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• In Vitro:
  Salinomycin, a potent Wnt signaling cascade inhibitor and antibiotic potassium ionophore, demonstrates significant anticancer properties. It induces apoptosis in malignant lymphocytes within 48 hours, showing a mean IC50 value of 230 nM. Notably, Salinomycin has been identified as a selective inhibitor of breast cancer stem cells (CSCs), effectively inhibiting both normal and Cisp-resistant SW620 cancer cells with IC50 values of 1.54±0.23 μM and 0.32±0.05 μM, respectively. It uniquely targets and kills CSCs and therapy-resistant cancer cells. Continuous treatment with Salinomycin over 48 hours increases the apoptotic cell count significantly in Cisp-resistant SW620 cells compared to non-resistant SW620 cells, as observed under a microscope and confirmed through flow cytometric analysis of cell apoptosis. The apoptotic rate is markedly higher in Cisp-resistant SW620 cells (37.82±3.63%) than in standard SW620 cells (16.78±2.56%) (p<0.05).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

beta-catenin, betacatenin, bcatenin, Antibacterial, βcatenin, Salinomycin, Wnt/b-catenin, Wnt, Procoxacin, Wnt/β-catenin, Wnt/betacatenin

Compound Identifiers

PubChem CID

3085092