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.
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB231, MDA-MB468, HeLa and K562 cell lines |
| Preparation method | 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. |
| Concentrations | ~40 μM |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 322.42 |
| Formula | C19H18N2OS |
| CAS Number | 1001753-24-7 |
| Solubility (25°C) | 64 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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