SecinH3

SecinH3 is a selective inhibitor of cytohesins, blocking human, mouse, and Drosophila cytohesins with IC₅₀ values of 2.4 to 5.6 µM.¹ It binds the Sec7 domain of these small Arf-GEFs but does not bind Sec7 domains of larger Arf-GEFs.² In human liver carcinoma HepG2 cells, SecinH3 prevents cytohesin-dependent insulin signaling.¹ In mice, SecinH3 produces hepatic insulin resistance.¹ Inhibition of the cytohesin GEF from Drosophila, Steppke, blocks insulin signaling and interferes with development.³ SecinH3 is useful for studying the diverse roles of cytohesins, including the regulation of receptor-mediated cancer cell proliferation.⁴

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1. Hafner, M., Schmitz, A., Grüne, I., et al. Inhibition of cytohesins by SecinH3 leads to hepatic insulin resistance. Nature 444(7121), 941-944 (2006).

2. Bi, X., Schmitz, A., Hayallah, A.M., et al. Affinity-based labeling of cytohesins with a bifunctional SecinH3 photoaffinity probe. Angew. Chem. Int. Ed. Engl. 47(49), 9565-9568 (2008).

3. Fuss, B., Becker, T., Zinke, I., et al. The cytohesin Steppke is essential for insulin signalling in Drosophila. Nature 444(7121), 945-948 (2006).

4. Pan, T., Sun, J., Hu, J., et al. Cytohesins/ARNO: The function in colorectal cancer cells. PLoS One 9(3), e90997 (2014).

Singh, S.R., Zeng, X., Zhao, J., et al. The lipolysis pathway sustains normal and transformed stem cells in adult Drosophila. Nature 538(7623), 109-113 (2016).