373270
Hec1/Nek2 Mitotic Pathway Inhibitor I, INH1
N-(4-(2,4-Dimethylphenyl)-thiazol-2-yl)-benzamide, INH1, Inhibitor of Nek2/Hec1-1
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15 February 2012
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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.
| Product information | |||
|---|---|---|---|
| Form | White solid | ||
| Molar mass | 308.4 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥97% by HPLC | ||
| Solubility | DMSO or EtOH | ||
| Chemical formula | C18H16N2OS | ||
| CAS number | 313553-47-8 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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