INH154 is a potent Nek2 and Hec1 binding (INH) inhibitor with IC50s of 120 nM in MB468 cells and 200 nM in Hela cells for INH.

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

INH154 also suppresses the growth of leukemia, osteosarcoma, and glioblastoma cells.INH154 is highly potent in treating breast tumors with co-elevated expression of Hec1 and Nek2. INH154 is the most potent inhibitor of tumor cell growth. The IC50 values of INH154 in HeLa and MDA-MB-468 cancer cells are 0.20 and 0.12 μM, respectively.

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].