NSC23766

NSC23766 is a small molecule inhibitor that selectively blocks the interaction between Rac1, a Rho family GTPase, and its specific guanine nucleotide exchange factors (GEFs) such as Tiam1 and TrioN, thereby preventing Rac1 activation[1][3][4][9]. The compound acts as a competitive inhibitor at the Rac1-GEF interface and does not significantly affect the related GTPases Cdc42 or RhoA[1][3]. NSC23766 inhibits Rac1-driven processes including cell proliferation, migration, and invasion, and has been shown to reverse tumor phenotypes in cancer cell models and inhibit tumor progression and metastasis in animal models[1][3][8]. Additionally, it impairs various functions in neuronal cells (including modulation of pCREB signaling and NMDAR currents) and displays some off-target effects, such as antagonism of muscarinic acetylcholine receptors (mAChRs)[5][6][7]. Notably, preclinical studies report antiviral effects against influenza virus replication and anti-inflammatory properties[11]. NSC23766 is widely used in research but not approved for clinical use in humans. It was initially developed by the Children's Hospital Research Foundation[12].

Other names

N(6)-[2-[[4-(diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride