INH1

INH1 is an inhibitor of the interaction between the oncogene high expression in cancer 1 (Hec1) and its regulator, the serine/threonine kinase Nek2.¹ It binds to Hec1 and reduces Nek2 protein levels in HeLa cells when used at a concentration of 25 µM. INH1 inhibits the growth of MDA-MB-468, SK-BR-3, T47D, MDA-MB-361, ZR-75-1, HBL-100, MDA-MB-435, and Hs 578T breast cancer cells (GI₅₀s = 10.5-20.5 µM). It inhibits migration of MDA-MB-231 cells in a transwell migration assay (IC₅₀ = 176 nM).² INH1 (50 and 100 mg/kg) reduces tumor growth in an MDA-MB-468 mouse xenograft model.¹

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1. Wu, G., Qiu, X.-L., Zhou, L., et al. Small molecule targeting the Hec1/Nek2 mitotic pathway suppresses tumor cell growth in culture and in animal. Cancer Res. 68(20), 8393-8399 (2008).

2. Zheng, S., Zhong, Q., Jiang, Q., et al. Discovery of a series of thiazole derivatives as novel inhibitors of metastatic cancer cell migration and invasion. ACS Med. Chem. Lett. 4(2), 191-196 (2013).