373270

Hec1/Nek2 Mitotic Pathway Inhibitor I, INH1

The Hec1/Nek2 Mitotic Pathway Inhibitor I, INH1, also referenced under CAS 313553-47-8, controls the biological activity of Hec1/Nek2 Mitotic Pathway.

• Synonym(e): Hec1/Nek2 Mitotic Pathway Inhibitor I, INH1, Inhibitor of Nek2/Hec1-1, N-(4-(2,4-Dimethylphenyl)-thiazol-2-yl)-benzamide, INH1, N-(4-(2,4-Dimethylphenyl)-thiazol-2-yl)-benzamide, INH1, Inhibitor of Nek2/Hec1-1
• Empirische Formel (Hill-System): C₁₈H₁₆N₂OS
• CAS-Nummer: 313553-47-8
• Molekulargewicht: 308.40
• MDL number: MFCD01356769
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥97% (HPLC)
• Form: solid
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Eigenschaften

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: white
• solubility: DMSO: 50 mg/mL, ethanol: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [s]1c(nc(c1)c3c(cc(cc3)C)C)NC(=O)c2ccccc2
• InChI: 1S/C18H16N2OS/c1-12-8-9-15(13(2)10-12)16-11-22-18(19-16)20-17(21)14-6-4-3-5-7-14/h3-11H,1-2H3,(H,19,20,21)
• InChI key: JPMOKRWIYQGMJL-UHFFFAOYSA-N

Beschreibung

General description

A cell-permeable thiazolyl benzamide compound that directly binds Hec1 and disrupts Hec1/Nek2 complex formation, resulting in defective Hec1 kinetochores localization and cellular Nek2 destabilization/downregulation. Shown to induce a transient mitotic arrest in HeLa cultures and inhibit the proliferation of 10 breast cancer cell lines (GI₅₀ of 10-21 µM) as well as the cervical HeLa and colon HCT116 cancer lines, while exhibiting reduced potency against the noncancerous MCF10A line (GI₅₀ = 41 µM). Reported to suppress the MDA-MB-468-derived tumor growth (by ~53% and ~75% 3 wks after a 7-wk treatment period with 50 mg/kg and 100 mg/kg INH1, repectively, i.p.) in a murine breast cancer model in vivo.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Wu, G., et al. 2008. Cancer Res.68, 8393.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable