INH154

Research use only, not for human use.

INH154?is a novel small molecules disrupting Hec1/Nek2 interaction.

INH154?is a novel small molecules disrupting Hec1/Nek2 interaction, inhibits HeLa and MDA-MB-468 cancer cells growth with IC50 of 0.20 and 0.12 uM, respectively; suppresses the growth of leukemia, osteosarcoma, and glioblastoma cells, but has no significant growth inhibitory effects on non-tumorigenic fibroblast, HS27 and mammary epithelial cells; triggers Nek2 degradation and eventually cell death, suppresses tumor growth in mice without obvious toxicity.

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. INH154 also suppresses the growth of leukemia, osteosarcoma, and glioblastoma cells.

Tumor growth rates in mice treated with INH154 are evidently slower than those in control animals in a dose-dependent manner. In agreement with the tumor-growth data, the tumor proliferation index, determined by measuring BrdU staining, is clearly reduced in residual tumors treated with INH154 in comparison with vehicle alone. The expression levels of Nek2 and Hec1 S165 phosphorylation are also substantially reduced in INH154-treated tumors than in vehicle-treated tumors. On the other hand, mice body weights are measured during the 6.5 weeks treatment period and show little difference among treated and control groups. In addition, the toxicity of INHs by treating normal BALB/c ByJNarl mice with high dosage of INH154 (20 mg/kg) shows no significant difference of body weights, blood chemistry, and complete blood count (CBC) analysis among these groups of animals.

INH 154

Cell Cycle/DNA Damage

Hec1/Nek2

Hec1/Nek2

——

——

1587705-63-2

392.521

C22H24N4OS

>98% (HPLC)

DMSO : 62.5 mg/mL 159.23 mM; H2O : < 0.1 mg/mL

CC1=CC(=CC(=C1C2=CSC(=N2)NC(=O)C3=CC=NC=C3)C)N4CCCCC4

N-(4-(2,6-dimethyl-4-(piperidin-1-yl)phenyl)thiazol-2-yl)isonicotinamide

(-20℃)

With Ice Pack

≥ 2 years