INH154

SKU: orb1309546

Description

INH154 is a potent small molecule inhibitor targeting the Nek2-Hec1 interaction, exhibiting IC50 values of 120 nM in MB468 cells and 200 nM in Hela cells. It serves as a valuable research tool for studying mitotic regulation and has been utilized in both in vitro and in vivo cancer model studies to investigate potential anti-tumor mechanisms.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1587705-63-2
• MW: 392.52
• Purity: 99.95% (May vary between batches)
• Formula: C₂₂H₂₄N₄OS
• SMILES: Cc1cc(cc(C)c1-c1csc(NC(=O)c2ccncc2)n1)N1CCCCC1
• Target: Others,MAPK
• Solubility: H2O:< 0.1 mg/mL (insoluble);DMSO:65 mg/mL (165.6 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (12.74 mM)

Bioactivity

• Target IC50:
  INH:120 nM(MB468 cells)|INH:200 nM(Hela cells)
• In Vivo:
  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.
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• In Vitro:
  INH154 effectively inhibits the proliferation of leukemia, osteosarcoma, and glioblastoma cells and demonstrates high potency in treating breast tumors characterized by elevated levels of Hec1 and Nek2. It stands out as the most potent suppressor of tumor cell growth among its class, with IC50 values of 0.20 μM in HeLa cancer cells and 0.12 μM in MDA-MB-468 cancer cells, showcasing its exceptional effectiveness.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, INH, INH 154, INH154, INH-154, INH in Hela cells, INH in MB468 cells, Inhibitor

Compound Identifiers

PubChem CID

91669222