INH154 is a highly potent inhibitor of Nek2 and Hec1 binding (INH), with IC50 values of 120 nM in MB468 cells and 200 nM in Hela cells.

INH:120 nM(MB468 cells), INH:200 nM(Hela cells)

INH154 effectively inhibits the proliferation of leukemia, osteosarcoma, and glioblastoma cells and demonstrates high potency in treating breast tumors characterized by elevated levels of Hec1 and Nek2. It stands out as the most potent suppressor of tumor cell growth among its class, with IC50 values of 0.20 μM in HeLa cancer cells and 0.12 μM in MDA-MB-468 cancer cells, showcasing its exceptional effectiveness.

Tumor growth in mice treated with INH154 was significantly slower than in control animals in a dose-dependent manner. Consistent with tumor growth data, residual tumors treated with INH154 had significantly lower tumor proliferation index compared to vehicle alone. The expression levels of Nek2 and Hec1 S165 phosphorylation were also significantly reduced in INH154-treated tumors compared with vehicle-treated tumors. On the other hand, the body weight of the mice was measured during the 6.5-week treatment period, and there was little difference between the treated and control groups[1].