SecinH3

製品コードS7685 バッチS768501

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H20N4O4S
分子量 460.5 CAS No. 853625-60-2
Solubility (25°C)* 体外 DMSO 92 mg/mL (199.78 mM)
Ethanol 1 mg/mL warmed with 50ºC water bath (2.17 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 SecinH3 is a selective cytohesin inhibitor with IC50 of 2.4 μM, 5.4 μM, 5.4 μM, 5.6 μM, 5.6 μM, and 65 μM for hCyh2, hCyh1, mCyh3, hCyh3, drosophila steppke, and yGea2-S7, respectively.
in vitro In HepG2 cells, SecinH3 inhibits insulin signaling and associated gene expression. [1] SecinH3 also markedly inhibits migration of preadipocyte 3T3-L1 cells. [2] In the A549 cells, SecinH3 results in reduced proliferation by indirectly attenuating EGFR activation, and causes a synergistic antiproliferative effect when used in combination with gefitinib. [3]
in vivo In mice, SecinH3 increases the expression of gluconeogenic genes, reduces the expression of glycolytic, fatty acid and ketone body metabolism genes in the liver, reduces liver glycogen stores, and increases plasma insulin. [1] In mice bearing H460 xenografts, SecinH3 significantly retards tumor growth through its antiproliferative and pro-apoptotic effect. [3]

プロトコル(参考用のみ)

キナーゼアッセイ Aptamer displacement screen
A library of small molecules screened in duplicate from Comgenex (10000 molecules) in 386 well plates by fluorescence polarization at an excitation wavelength of 485 nm using read-out at 520 nm in a reaction volume of 50 μL at 37° C. The screening buffer is PBS, pH 7.5, 3 mM MgCl2, 100 nM fluorecein-labelled M69 aptamer, 1 μM cytohesin-1 Sec7 at 100 μM compound concentrations.
細胞アッセイ 細胞株 NSCLC A549 and H460 cell lines
濃度 ~15 μM
反応時間 72 hours
実験の流れ 3×103 cells per 96 well are seeded into a clear, flat bottom 96 well plate (TPP). After 24 h the cells are treated with the indicated concentrations of the inhibitors or solvent (final DMSO concentration 0.4%) in RPMI containing 50 ng/mL EGF or IGF-1, respectively. Medium is changed daily for 3 days and cell proliferation is analyzed with a MTT assas as described in the manufacturer’s protocol using a Varioscan microplate reader. All assays are performed at least in triplicates.
動物実験 動物モデル Mice bearing H460 xenografts
投薬量 100 μL 2.5 mM, once daily
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , J Exp Clin Cancer Res, 2017, 36(1):112]

Data from [Data independently produced by , , IUBMB Life, 2018, 71(2):192-199]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Blocking the cytohesin-2/ARF1 axis by SecinH3 ameliorates osteoclast-induced bone loss via attenuating JNK-mediated IRE1 endoribonuclease activity [ Pharmacol Res, 2022, 185:106513] PubMed: 36252772
Genome-wide CRISPR-Cas9 screening identifies the CYTH2 host gene as a potential therapeutic target of influenza viral infection [ Cell Rep, 2022, 38(13):110559] PubMed: 35354039
SecinH3 Attenuates TDP-43 p.Q331K-Induced Neuronal Toxicity by Suppressing Endoplasmic Reticulum Stress and Enhancing Autophagic Flux [Hu W, et al. IUBMB Life, 2018, 71(2):192-199] PubMed: 30376609
Combined targeting of Arf1 and Ras potentiates anticancer activity for prostate cancer therapeutics. [Lang L, et al. J Exp Clin Cancer Res, 2017, 36(1):112] PubMed: 28830537

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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