| Identification | Back Directory | [Name]
INH154 | [CAS]
1587705-63-2 | [Synonyms]
INH154
INH154,inhibit,Inhibitor,INH-154,INH 154
4-Pyridinecarboxamide, N-[4-[2,6-dimethyl-4-(1-piperidinyl)phenyl]-2-thiazolyl]- | [Molecular Formula]
C22H24N4OS | [MDL Number]
MFCD31746890 | [MOL File]
1587705-63-2.mol | [Molecular Weight]
392.52 |
| Chemical Properties | Back Directory | [density ]
1.248±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:81.17(Max Conc. mg/mL);206.78(Max Conc. mM)
Ethanol:5.0(Max Conc. mg/mL);12.74(Max Conc. mM) | [form ]
Solid | [pka]
5.39±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
INH154 is a highly potent inhibitor for Nek2 and Hec1 binding (INH), with IC50s of 200 nM and 120 nM for INH in Hela and MB468 cells. | [in vivo]
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[1]. | [IC 50]
NEK2 | [References]
[1] Hu CM, et al. Novel small molecules disrupting Hec1/Nek2 interaction ablate tumor progression by triggering Nek2 degradation through a death-trap mechanism. Oncogene. 2015 Mar 5;34(10):1220-30. DOI:10.1038/onc.2014.67 |
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