MBQ-167

MBQ-167 (MBQ167) is a dual inhibitor of Rac/Cdc42 (Ras-related C3 botulinum toxin substrate and cell division control protein 42 homolog) with anticancer activity. In metastatic MDA-MB-231 cells, it inhibits Rac 1/2/3 and Cdc42 with IC50 values of 103 nM and 78 nM, respectively. Thus, without influencing the activities of Rho, MAPK, or Akt, MBQ-167 dramatically reduces the downstream effector p21-activated kinase (PAK) signaling and the activity of STAT3. Additionally, MBQ-167 prevents the migration, viability, and formation of mammospheres in breast cancer cells. Additionally, MBQ-167 inhibits actin-based extensions on the cell surface and causes a loss of cell polarity in cancer cells that have undergone the epithelial-to-mesenchymal transition, which ultimately leads to the cells' separation from the substratum. Extended (120 h) incubation in MBQ-167 reduces the viability of metastatic cancer cells with a GI50 of about 130 nmol/L, while having no effect on mammary epithelial cells that are not cancerous. Cancer cell viability is lost as a result of G2-M cell-cycle arrest mediated by MBQ-167 and subsequent apoptosis, particularly of the detached cells. In immunocompromised mice, MBQ-167 inhibits the growth and metastasis of mammary tumors by about 90% in vivo. Finally, MBQ-167 has the potential to be developed as an anticancer medication and a dual inhibitory probe for the study of Rac and Cdc42 because it is 10× more potent than other Rac/Cdc42 inhibitors that are currently on the market.

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.