N-[4-(2,4-ジメチルフェニル)-2-チアゾリル]ベンズアミド

一般的な説明A cell-permeable thiazolyl benzamide compound that directly binds Hec1 and disrupts Hec1/Nek2 complex formation, resulting in defective Hec1 kinetochores localization and cellular Nek2 destabilization/downregulation. Shown to induce a transient mitotic arrest in HeLa cultures and inhibit the proliferation of 10 breast cancer cell lines (GI50 of 10-21 μM) as well as the cervical HeLa and colon HCT116 cancer lines, while exhibiting reduced potency against the noncancerous MCF10A line (GI50 = 41 μM). Reported to suppress the MDA-MB-468-derived tumor growth (by ~53% and ~75% 3 wks after a 7-wk treatment period with 50 mg/kg and 100 mg/kg INH1, repectively, i.p.) in a murine breast cancer model in vivo.