GC-7

GC7 Sulfate is a deoxyhypusine synthase (DHPS) inhibitor. IC50 & Target:DHPS^[1] In Vitro:The treatment of MYCN2 (±Dox) and BE(2)-C cells with GC7 for 72 h at various concentrations (0.1 to 100 μM) significantly reduces the number of viable cells in a dose-dependent manner. In MYCN2 cells, 5 μM of GC7 inhibits cell viability by ~40 and ~60 %, respectively, compare to untreated control cells. BE(2)-C cells require 25 μM of GC7 to reduce cell viability by ~50 %. Exposure to 10 and 100 μM GC7 for 72 h clearly decreases the levels of total retinoblastoma (Rb) and phosphorylated Rb as well as of Cdk4 protein, and increases the levels of p21 protein^[1]. Between 0 and 20 μM, GC7 induces little cytotoxicity in HCC cells, while higher concentrations of GC7 (50 to 100 μM) significantly inhibit the viability of all five HCC cell lines tested. Newly synthesized ³H-labeled hypusine of eIF5A1/eIF5A2 is rarely detected after 20 μM GC7 treatment, compare to untreated control. The activity of [³H]-spermidine incorporated into HCC cells is significantly decreased by 20 μM GC7 or higher concentration^[2].