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].

Product Specifications

CAS Number

[1637739-82-2]

UNSPSC

12352005

Hazard Statement

H302, H312, H315, H319, H332, H335

Target

Ras

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/BQU57.html

Purity

99.45

Solubility

DMSO : ≥ 100 mg/mL

Smiles

NC1=C(C#N)C(C(C(C)=NN2C)=C2O1)C3=CC=C(C(F)(F)F)C=C3

Molecular Formula

C16H13F3N4O

Molecular Weight

334.30

Precautions

H302, H312, H315, H319, H332, H335

References & Citations

[1]Yan C, et al. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515 (7527) :443-447.|[2]Qiu X, et al. BQU57 suppresses IL-1β-induced apoptosis and extracellular matrix degradation in nucleus pulposus cells by blocking the NF-κB signaling pathway. Cell Signal. 2025 Mar 8:111729.|[3]Thies KA, et al. The small G-protein RalA promotes progression and metastasis of triple-negative breast cancer. Breast Cancer Res. 2021 Jun 12;23 (1) :65.