RKN5755
RKN5755 is a β-arrestin1 inhibitor and a selective inhibitor of activated fibroblasts. RKN5755 binds to β-arrestin1 and interferes with the cofilin signaling pathway mediated by this protein to block its function. RKN5755 not only inhibits the enhanced migratory effect of fibroblasts co-cultured with cancer cells, but also prevents the inhibitory effect of EP3 agonists on the EP2 receptor-induced elevation of tetrodotoxin-resistant sodium currents in mouse dorsal root ganglion neurons. RKN5755 is widely used in research on related diseases such as cancer metastasis and pain.
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- CAS. Nr.: 1005056-10-9
- Formel: C14H16O3
- Molecular Weight:232.28
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Arrestin-2/β-Arrestin 1 |
In Vitro
RKN5755 (3-6 μM; 24 h) inhibits the enhanced migration of NIH3T3 mouse embryonic fibroblasts cocultured with MCF7 human breast cancer cells, without affecting migration of NIH3T3 cells cultured alone[1].
RKN5755 (3-6 μM; 12 h) inhibits the enhanced transwell migration of NIH3T3 mouse embryonic fibroblasts cocultured with MCF7 human breast cancer cells, without affecting migration of NIH3T3 cells cultured alone[1].
RKN5755 (0.3-6 μM; 48 h) does not inhibit proliferation of NIH3T3 mouse embryonic fibroblasts or MCF7 human breast cancer cells[1].
RKN5755 (6 μM; 24 h) inhibits the enhanced migration of WI-38 human lung fibroblasts cocultured with MCF7 human breast cancer cells[1].
RKN5755 (1-6 μM; 24 h) inhibits cofilin activation (dephosphorylation at Ser3) in NIH3T3 mouse embryonic fibroblasts cocultured with MCF7 human breast cancer cells in a dose-dependent manner, restoring inactive phospho-Ser3-cofilin levels to those of NIH3T3 cells cultured alone at 6 μM[1].
RKN5755 (10 μM) prevents the EP3 agonist-mediated inhibition of EP2 receptor-induced increases in maximal TTX-R Na+ current amplitudes in small- to medium-sized wild-type mouse DRG neurons[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:NIH3T3 mouse embryonic fibroblasts, MCF7 human breast cancer cells
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Concentration:0.3-6 μM
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Incubation Time:48 h
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Result:Did not inhibit proliferation of NIH3T3 or MCF7 cells at any tested concentration.
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Cell Line:NIH3T3 mouse embryonic fibroblasts, MCF7 human breast cancer cells
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Concentration:1-6 μM
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Incubation Time:24 h
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Result:Increased phospho-Ser3-cofilin levels in a dose-dependent manner.
Restored phospho-Ser3-cofilin levels to those seen in NIH3T3 cells cultured alone at 6 μM, indicating complete inhibition of cofilin activation.
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Cell Line:NIH3T3 mouse embryonic fibroblasts, MCF7 human breast cancer cells
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Concentration:0.3-6 μM
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Incubation Time:48 h
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Result:Had no inhibitory effect on the proliferation of either NIH3T3 or MCF7 cells at concentrations up to 6 μM.
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Cell Line:NIH3T3 mouse embryonic fibroblasts, MCF7 human breast cancer cells
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Concentration:1-6 μM
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Incubation Time:24 h
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Result:Increased Ser3-phosphorylated cofilin levels in a dose-dependent manner in cocultured NIH3T3 cells.
Restored phosphorylated cofilin levels to those of NIH3T3 cells cultured alone at 6 μM, indicating complete inhibition of coculture-induced cofilin activation.
Chemical Information
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CAS. Nr. 1005056-10-9
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Molecular Weight 232.28
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Formel C14H16O3
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SMILES
OC(C1CCC2)(OC(C1)=O)C2C3=CC=CC=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Primary Dorsal Root Ganglion Sensory Neuron Culture
Primary dorsal root ganglion sensory neuron culture isolates DRG neuronal somata from rodent or human ganglia, dissociates tissue enzymatically and mechanically, and maintains post-mitotic sensory neurons in vitro for readouts such as neurite outgrowth, immunocytochemical marker expression, calcium imaging, electrophysiology, RNA/protein analysis, or neuropeptide release assays. The method reflects peripheral sensory neuron biology because DRG neurons are primary sensory neurons whose cell bodies reside in dorsal root ganglia and whose cultured dissociated cells can retain neuronal morphology, sensory-neuron marker expression, and stimulus-responsive properties depending on the downstream assay.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Reinheit & Dokumentation
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Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)