1A-116

1A-116 is an inhibitor of Rac1 (IC₅₀ = 4 µM).¹ It reduces the secretion of chemokine (C-X-C motif) ligand 5 (CXCL5), CXCL10, hepatocyte growth factor (HGF), chemokine (C-C motif) ligand 2 (CCL2), and matrix metalloproteinase-2 (MMP-2) from patient-derived acute myeloid leukemia (AML) cells when used at a concentration of 20 µM.² 1A-116 (20 µM) inhibits the proliferation and migration of, and induces apoptosis in, LN-229 glioblastoma cells at 10 hours, but not 23 hours, post-synchronization.³ In vivo, IA-116 (3 mg/kg per day) decreases the number of lung nodules and macronodules, as well as total lung weight, in a F3II murine breast cancer model of lung tumor formation.¹ It also inhibits the asexual replication of the P. falciparum strains D10 and W2 (IC₅₀s = 3.21 and 6.89 µM, respectively) and sexual replication in P. falciparum 3D7 immature and mature gametocytes (IC₅₀s = 78.13 and 56.64 µM, respectively).⁴

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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. Hemsing, A.L., Rye, K.P., Hatfield, K.J., et al. NPM1-mutated patient-derived AML cells are more vulnerable to Rac1 inhibition. Biomedicines 10(8), 1881 (2022).

3. Trebucq, L.L., Cardama, G.A., Lorenzano Menna, P., et al. Timing of novel drug 1A-116 to circadian rhythms improves therapeutic effects against glioblastoma. Pharmaceutics 13(7), 1091 (2021).

4. 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).