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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 1005056-10-9
分子式: C₁₄H₁₆O₃
分子量:232.28

保管条件:

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

RKN5755 構造式

CAS 番号: 1005056-10-9

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性

製品説明

IC₅₀ & Target^[1]

Arrestin-2/β-Arrestin 1

Arrestin アイソフォーム固有の製品をすべて表示 :

体外実験

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.

化学情報

CAS 番号 1005056-10-9
分子量 232.28
分子式 C₁₄H₁₆O₃
SMILES

OC(C1CCC2)(OC(C1)=O)C2C3=CC=CC=C3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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.

Calculators

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希釈計算機

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Help & FAQs

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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MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
化学情報
純度とドキュメンテーション
参考文献

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製品番号:
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RKN5755

Arrestin アイソフォーム固有の製品をすべて表示