MBQ-167

MBQ-167 is a dual inhibitor of Rac and cell division cycle 42 (Cdc42; IC₅₀s = 103 and 78 nM, respectively).¹ It reduces Rac and Cdc42 GTP binding and GTPase activity and limits migration and mammosphere formation in MDA-MB-231 breast cancer cells when used at a concentration of 250 nM. MBQ-167 (250 nM), alone and in combination with the kinase inhibitor lapatinib (Item No. 11493), reduces cell viability and induces apoptosis in lapatinib-resistant SK-BR-3 and MDA-MB-435 breast cancer cells.² It also reduces growth rates, axial budding, and Cdc42 activity in S. cerevisiae when used at a concentration of 200 µM.³ Intraperitoneal administration of MBQ-167 (1 or 10 mg/kg three times per week) reduces tumor growth in an MDA-MB-435 mouse xenograft model.¹

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1. Humphries-Bickley, T., Catstillo-Pichardo, L., Hernandez-O'Farrill, E., et al. Characterization of a dual Rac/CDC42 inhibitor MBQ-167 in metastatic cancer. Mol. Cancer Ther. 16(5), 805-818 (2017).

2. Borrero-Garcia, L.D., Maldonado, M.D.M., Medina-Velazquez, J., et al. Rac inhibition as a novel therapeutic strategy for EGFR/HER2 targeted therapy resistant breast cancer. BMC Cancer 21(1), 652 (2021).

3. Rivera-Robles, M.J., Medina-Valazquez, J., Asencio-Torres, G.M., et al. Targeting Cdc42 with the anticancer compound MBQ-167 inhibits cell polarity and growth in the budding yeast S. cerevisiae. Small GTPases 11(6), 430-440 (2020).