(E)-FOBISIN101 is a 14-3-3 protein-protein interaction ( 14-3-3 protein-protein interaction ) inhibitor, with IC50 values of 9.3 and 16.4 μM for disrupting the binding of 14-3-3ζ or 14-3-3γ to PRAS40, respectively. (E)-FOBISIN101 inhibits the binding of 14-3-3 to Raf-1 and proline-rich AKT substrate, and neutralizes the ability of 14-3-3 to activate exotoxin S ADP-ribosyltransferase. (E)-FOBISIN101 is applicable to 14-3-3-mediated cancer research [1].
In Vitro, FOBISIN101 (5 mM; 3 days) forms a covalent adduct with Lys120 in purified 14-3-3ζ after X-ray radiation, occupying the peptide-binding groove and inactivating the protein[1].
References:
[1]. Zhao J, et al. Discovery and structural characterization of a small molecule 14-3-3 protein-protein interaction inhibitor. Proceedings of the National Academy of Sciences. 2011 Sep 27;108(39):16212-6.
In Vitro, FOBISIN101 (5 mM; 3 days) forms a covalent adduct with Lys120 in purified 14-3-3ζ after X-ray radiation, occupying the peptide-binding groove and inactivating the protein[1].
References:
[1]. Zhao J, et al. Discovery and structural characterization of a small molecule 14-3-3 protein-protein interaction inhibitor. Proceedings of the National Academy of Sciences. 2011 Sep 27;108(39):16212-6.