SecinH3 is selective cytohesin inhibitor.

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

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 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]

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)