INH154 是一种高效的 Nek2 和 Hec1 结合抑制剂，能够抑制 Hela 细胞(IC50:200 nM)、 MB468 细胞(IC50:120 nM)。

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.

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].

1587705-63-2

C22H24N4OS

392.52

DMSO:75 mg/mL (191.07 mM),Need ultrasonic
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years