BQU57

BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity^[1][2][3]. In Vitro:BQU57 inhibits RalA/RalB activated H2122 and H358 lung cancer cell clones with IC₅₀s of 2.0 μM (H2122) and 1.3 μM (H358), respectively^[1].
BQU57 (5 μM and 10 μM; 24 h) reduces rat nucleus pulposus cell apoptosis and mitochondrial dysfunction and maintains extracellular matrix (ECM) metabolic balance by inhibiting IL-1β-induced nuclear factor κB (NF-κB) signaling pathway^[2].
BQU57 (50 μM; 72 h) significantly reduces triple-negative breast cancer (TNBC) cell viability, inhibited its migration and invasion ability, and reduced non-adherent growth by blocking the RalA/RalB signaling pathway^[3].
BQU57 (100 μM; 72 h) combined with Paclitaxel produced a synergistic toxic effect on TNBC cells and enhanced chemotherapy sensitivity^[3]. In Vivo:BQU57 (1 mg/kg and 5 mg/kg; ip; once a day; 6 weeks) significantly alleviated lumbar instability-induced disc degeneration in rats, reduced nucleus pulposus cell apoptosis and maintained disc structural integrity^[2].
BQU57 (50 mg/kg; ip; 3 times a week; 21 days) significantly inhibited orthotopic tumor growth and lung metastasis in mice with triple-negative breast cancer (TNBC) and prolonged survival^[3].