SecinH3 is selective cytohesin inhibitor.

Cyh3 (human):5.6 μM, Cyh1 (human):5.4 μM, Cyh3 (mouse):5.4 μM, Cyh2 (human):2.4 μM, Drosophila steppke:5.6 μM

在HepG2细胞中，SecinH3抑制胰岛素信号传导及其相关基因的表达。[1] SecinH3还显著抑制前脂肪细胞3T3-L1的迁移。[2] 在A549细胞中，SecinH3通过间接减弱EGFR激活，降低细胞增殖，并且与gefitinib联用时产生协同抗增殖效应。[3]

在小鼠体内，SecinH3提升糖异生基因的表达，降低肝脏中的糖酵解、脂肪酸及酮体代谢基因的表达，减少肝脏糖原储存，并提高血浆胰岛素水平。[1] 对携带H460异种移植瘤的小鼠而言，SecinH3通过其抗增殖和促凋亡效应显著地延缓肿瘤生长。[3]

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.

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. (Only for Reference)