product name INH6
Description: INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment. INH6 inhibited Hec1/Nek2 function through protein degradation that led to chromosome mis-segregation and cell death. In MDA-MB468 and MDA-MB231 human breast cancer cell lines, HeLa human cervical cancer line and K562 human erythromyeloblastoid leukemia cell line, INH6 exhibited significantly anti-proliferation activities with IC50 values of 2.1, 1.7, 2.4 and 2.5 µM, respectively.
References: J Med Chem. 2009 Mar 26;52(6):1757-67.
322.42
Formula
C19H18N2OS
CAS No.
1001753-24-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 64 mg/mL (198.5 mM)
Water: <1 mg/mL
Ethanol: 11 mg/mL (34.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: INH6 effectively targets the Hec1/Nek2 complex for degradation, and shows potent cell killing activity with IC50 of 1.7, 2.1, 2.4, and 2.5 μM in MDA-MB231, MDA-MB468, HeLa and K562 cell lines. INH6 also triggers mitotic abnormalities in HeLa cells, and induces apoptosis. Kinase Assay: Cell Assay: Standard XTT assays with a four-day drug treatment procedure are performed to measure the dose-dependent cytotoxicity of INH analogs in cultured cells. Triplicate sets are measured and compiled for final data presentation. The assay is performed by using a commercial kit following the instructions. In principle, cells are plated on 96-well dishes one day before the drug treatment, followed by drug treatment on day 2 and XTT assay on day 5 after drug addition. The absorption at 595 nm is measured with a plate reader and converted to cell survival percentages in comparison to mock treated groups. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2009 Mar 26;52(6):1757-67. |
