ZINC69391

ZINC69391 is a small-molecule, specific inhibitor of the Ras-related C3 botulinum toxin substrate 1 (Rac1) GTPase. It acts by masking the Trp56 residue on the surface of Rac1, thereby disrupting its interaction with guanine nucleotide exchange factors (GEFs) such as Tiam1 and DOCK180. This blockade prevents Rac1 activation (reducing intracellular Rac1-GTP levels) and downregulates downstream signaling effectors like Pak1. ZINC69391 has demonstrated preclinical efficacy in inhibiting cell proliferation, migration, and invasion, as well as inducing cell cycle arrest and apoptosis in aggressive cancer models, including breast cancer and glioma. It has also shown in vivo antimetastatic activity by reducing lung colonization in experimental metastasis models.

Other names

N-(4,6-dimethyl-2-pyrimidinyl)-N'-[2-(trifluoromethyl)phenyl]-guanidine