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Cat. No.: HY-187689

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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 No.: 1005056-10-9
Formule: C₁₄H₁₆O₃
Masse moléculaire:232.28

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

RKN5755 Chemical Structure

CAS No.: 1005056-10-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références
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Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

Arrestin-2/β-Arrestin 1

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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.

Cell Proliferation Assay^[1]

Cell Line:

NIH3T3 mouse embryonic fibroblasts, MCF7 human breast cancer cells
Concentration:

0.3-6 μM
Incubation Time:

48 h
Result:

Did not inhibit proliferation of NIH3T3 or MCF7 cells at any tested concentration.

Western Blot Analysis^[1]

Cell Line:

NIH3T3 mouse embryonic fibroblasts, MCF7 human breast cancer cells
Concentration:

1-6 μM
Incubation Time:

24 h
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.

Cell Proliferation Assay^[2]

Cell Line:

NIH3T3 mouse embryonic fibroblasts, MCF7 human breast cancer cells
Concentration:

0.3-6 μM
Incubation Time:

48 h
Result:

Had no inhibitory effect on the proliferation of either NIH3T3 or MCF7 cells at concentrations up to 6 μM.

Western Blot Analysis^[2]

Cell Line:

NIH3T3 mouse embryonic fibroblasts, MCF7 human breast cancer cells
Concentration:

1-6 μM
Incubation Time:

24 h
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

CAS No. 1005056-10-9
Masse moléculaire 232.28
Formule C₁₄H₁₆O₃
SMILES

OC(C1CCC2)(OC(C1)=O)C2C3=CC=CC=C3
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Suvarna K, et al. Identification of a small-molecule ligand of β-arrestin1 as an inhibitor of stromal fibroblast cell migration accelerated by cancer cells. Cancer medicine. 2018 Mar;7(3):883-893.

[2]. König C, et al. Prostaglandin EP3 receptor activation is antinociceptive in sensory neurons via PI3Kγ, AMPK and GRK2. British journal of pharmacology. 2023 Feb;180(4):441-458.

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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RKN5755

Voir tous les produits spécifiques à Isoform Arrestin