INH154

CAS No. 1587705-63-2

INH154( INH 154 )

Catalog No. M12265 CAS No. 1587705-63-2

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    INH154
  • Note
    Research use only, not for human use.
  • Brief Description
    INH154?is a novel small molecules disrupting Hec1/Nek2 interaction.
  • Description
    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.
  • In Vitro
    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.
  • 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.
  • Synonyms
    INH 154
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    Hec1/Nek2
  • Recptor
    Hec1/Nek2
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1587705-63-2
  • Formula Weight
    392.521
  • Molecular Formula
    C22H24N4OS
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 62.5 mg/mL 159.23 mM; H2O : < 0.1 mg/mL
  • SMILES
    CC1=CC(=CC(=C1C2=CSC(=N2)NC(=O)C3=CC=NC=C3)C)N4CCCCC4
  • Chemical Name
    N-(4-(2,6-dimethyl-4-(piperidin-1-yl)phenyl)thiazol-2-yl)isonicotinamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Hu CM, et al. Oncogene. 2015 Mar 5;34(10):1220-30.
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