Description
Biochem/physiol Actions
BQU57 is a selective inhibitor of the Ras-like GTPases RalA and RalB, downstream mediators of Ras signalling, without direct inihibition of Ras or RhoA activity . BQU57 binds to a site on the GDP-bound form of Ral, its inactive state, inhibiting the binding of Ral to its effectors, such as Ral-binding protein 1 (RALBP1; also known as RLIP760, which are involved in proliferation, survival, and metastasis of several human cancers. BQU57 inhibited growth in human luung cancer cell lines with IC₅₀ values of 2.0 μM in H2122 cells and 1.3 μM in H358 cells, and also inihbited tumor xenograft growth.
BQU57 is a selective inhibitor of the Ras-like GTPases RalA and RalB.