同义名 :	-
	CAS号 :	853625-60-2
	货号 :	A923399
	分子式 :	C24H20N4O4S
	纯度 :	99%+
	分子量 :	460.5
	MDL号 :	MFCD10687099
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

SecinH3 is a selective cytohesin inhibitor for hCyh2, hCyh1, mCyh3, hCyh3, drosophila steppke, and yGea2-S7 with IC50 of 2.4 μM, 5.4 μM, 5.4 μM, 5.6 μM, 5.6 μM, and 65 μM respectively. SecinH3 almost completely blocks the insulin-dependent transcriptional repression of IGFBP1 with an IC50 of 2.2 μM. Insulin-stimulated translocation of ARF6 to the plasma membrane is also inhibited by SecinH3. SecinH3-treated mice show increased expression of gluconeogenic genes, reduced expression of glycolytic, fatty acid and ketone body metabolism genes in the liver, reduced liver glycogen stores, and a compensatory increase in plasma insulin[3]. SecinH3, a cytohesin inhibitor, has neuroprotective effects against mutant SOD1 toxicity. SecinH3 was demonstrated to successfully attenuate the TDP-43 (transactivating response region DNA binding protein 43) Q331K-induced neuronal toxicity by suppressing ER (endoplasmic reticulum) stress-mediated apoptosis and enhancing the autophagic flux[4]. SecinH3 can significantly inhibit the cytohesins and then relieve the lung injury induced by the sepsis of rats[5]. Treating mice bearing H460 xenografts with SecinH3 showed the antiproliferative and pro-apoptotic effect of SecinH3 in vivo[6].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.17mL 0.43mL 0.22mL	10.86mL 2.17mL 1.09mL	21.72mL 4.34mL 2.17mL

参考文献

[1]Torii T, Miyamoto Y, et al. Cytohesin-2/ARNO, through its interaction with focal adhesion adaptor protein paxillin, regulates preadipocyte migration via the downstream activation of Arf6. J Biol Chem. 2010 Jul 30;285(31):24270-81. [2]Hafner M, Schmitz A, et al. Inhibition of cytohesins by SecinH3 leads to hepatic insulin resistance. Nature. 2006 Dec 14;444(7121):941-4. [3]Hafner M, Schmitz A, Grüne I, Srivatsan SG, Paul B, Kolanus W, Quast T, Kremmer E, Bauer I, Famulok M. Inhibition of cytohesins by SecinH3 leads to hepatic insulin resistance. Nature. 2006 Dec 14;444(7121):941-4 [4]Hu W, Liu X, Wang S, Sun G, Zhao R, Lu H. SecinH3 Attenuates TDP-43 p.Q331K-Induced Neuronal Toxicity by Suppressing Endoplasmic Reticulum Stress and Enhancing Autophagic Flux. IUBMB Life. 2019 Feb;71(2):192-199 [5]Guo F, Yan CY. Effect of SecinH3 on lung injury induced by sepsis of rats. Asian Pac J Trop Med. 2015 Dec;8(12):1049-1054 [6]Bill A, Schmitz A, König K, Heukamp LC, Hannam JS, Famulok M. Anti-proliferative effect of cytohesin inhibition in gefitinib-resistant lung cancer cells. PLoS One. 2012;7(7):e41179