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Description

A cell-permeable triazolo compound that acts as a Sec7 domain-binding (Kd <=250 nM for Sec7 from human cytohesins 1-3), selective antagonist against cytohesin family small GEFs (IC50 <=5.6 µ,M in ARF1 GDP/GTP exchange assays using human cytohesin 3, as well as murine and Drosophila homologues). It inhibits large GEFs only at much higher concentrations (IC50 >=65 µ,M in GDP/GTP exchange assays using hEFA6-S7 and yGea2-S7) and exhibits little activity against a panel of 10 commonly studied kinases or hSosII. Shown to effectively inhibit insulin signaling both in HepG2 cells in vitro and in Drosophila and mice in vivo.