RBC8

Description: RBC8 is a novel and potent inhibitor of Ral GTPase with IC50 of 3.5 uM in H2122 cells and 3.4 uM in H358 cells. The Ras-like GTPases RalA and RalB are important drivers of tumour growth and metastasis. Chemicals that block Ral function would be valuable as research tools and for cancer therapeutics. RBC8 inhibited tumor growth to a similar extent as dual knockdown of RalA and RalB. RBC8 inhibited the binding of Ral to its effector RALBP1, as well as inhibiting Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines. RBC8 and BQU57 show selectivity for Ral relative to the GTPases Ras and RhoA and inhibit tumour xenograft growth to a similar extent to the depletion of Ral using RNA interference.

References: Nature. 2014 Nov 20; 515(7527):443-7.