ZINC69391

ZINC69391 is an inhibitor of the protein-protein interaction between Rac1 and the Rho guanine nucleotide exchange factor TIAM1.¹ It inhibits the interaction between Rac1 and TIAM1 in a cell-free assay when used at a concentration of 200 µM. ZINC69391 is also active against chloroquine-resistant and -susceptible strains of P. falciparum (IC₅₀ = 17.56 and 12.56, respectively).² It inhibits the proliferation of MDA-MB-231, F3II, and MCF-7 breast cancer cells (IC₅₀s = 48, 61, and 31 µM, respectively).¹ ZINC69391 (10 µM) induces cell cycle arrest at the G₁ phase in MDA-MB-231 cells. It inhibits EGF-induced actin polymerization in, and the migration and invasion of, MDA-MB-231 and F3II cells when used at a concentration of 50 µM. In vivo, ZINC69391 (25 mg/kg per day) reduces the number of lung nodules in an F3II murine model of lung metastasis when administered at a dose of 25 mg/kg per day.

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1. Cardama, G.A., Comin, M.J., Hornos, L., et al. Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines. Anticancer Agents Med. Chem. 14(6), 840-851 (2014).

2. Parapini, S., Paone, S., Erba, E., et al. In vitro antimalarial activity of inhibitors of the human GTPase Rac1. Antimicrob. Agents Chemother. 66(1), e0149821 (2022).