SecinH3

製品コードS7685 バッチS768501

印刷

化学情報

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 (warmed with 50ºC water bath)

1 mg/mL (2.17 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.500mg/ml (3.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.760mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 15.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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] This compound also markedly inhibits migration of preadipocyte 3T3-L1 cells. ^[2]
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, this compound 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
キナーゼアッセイ	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 this 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 this compound 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.

参考

https://pubmed.ncbi.nlm.nih.gov/17167487/
https://pubmed.ncbi.nlm.nih.gov/20525696/
https://pubmed.ncbi.nlm.nih.gov/22815959/

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。