NSC 668394

NSC 668394 is a binder of ezrin (K_d = 10.6 µM).¹ It inhibits PKCι-induced phosphorylation of ezrin in a cell-free assay (IC₅₀ = 8.1 µM).² NSC 668394 (10 µM) inhibits the interaction between ezrin and actin in K7M2 osteosarcoma cells. It inhibits the migration and invasion of K7M2 cancer cells when used at a concentration of 2 µM.¹ NSC 668394 (10 µM) reduces bacterial invasion but is not bactericidal in HEp-2 cells infected with group A Streptococcus (GAS).³ It induces developmental delays and cyclopia in Xenopus larvae when used at a concentration of 10 µM and induces toxicity at 40 µM.²

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1. Paige, M., Kosturko, G., Bulut, G., et al. Design, synthesis and biological evaluation of ezrin inhibitors targeting metastatic osteosarcoma. Bioorg. Med. Chem. 22(1), 478-487 (2014).

2. Bulut, G., Hong, S.-H., Chen, K., et al. Small molecule inhibitors of ezrin inhibit the invasive phenotype of osteosarcoma cells. Oncogene 31(3), 269-281 (2021).

3. Rox, K., Rohde, M., Chhatwal, G.S., et al. Disorazoles block group A streptococcal invasion into epithelial cells via interference with the host factor ezrin. Cell Chem. Biol. 24(2), 159-170 (2017).