IGGi-11me is a membrane permeable prodrug of IGGi-11, which is the first-in-class inhibitor of noncanonical activation of heterotrimeric G-protein signaling. IGGi-11 binding to G-protein α-subunits (Gαi) specifically disrupted their engagement with GIV/Girdin, thereby blocking noncanonical G-protein signaling in tumor cells and inhibiting proinvasive traits of metastatic cancer cells.

The membrane permeability of IGGi-11me was higher than that of IGGi-11. The esterase in the cytoplasm of MDA-MB-231 cells could convert IGGi-11me into IGGi-11. Thus, IGGi-11me acts as a prodrug, allowing IGGi-11 to function in cells much better.

KEYWORDS: IGGi-11me | Supplier | GIV-Gαi inhibitor | IGGi-11 prodrug | IGGi11me | IGGi 11me | GLXC27028 | GLXC 27028 | GLXC-27028 | CAS [N.A.] | GPCR-independent noncanonical G-protein signaling | Inhibitor | Enzymes | Heterotrimeric G-protein | GIV | Girdin | Tumor | Gα subunit