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BIX-01294 Trihydrochloride is a G9a-like protein and G9a histone lysine methyltransferase inhibitor with IC50 values of 0.7 and 1.7 μM respectively. BIX-01294 inhibits the G9aHMTase dependent levels of histone-3 lysine (9) methylation (H3K9me). BIX-01294 can also inhibit H3K9 Jumonji demethylase KIAA1718 with half-maximal inhibitory concentrations in low micromolar range. In its inhibition of the histone lysine methyltransferases, BIX 01294 does not compete with cofactor S-adenosyl-methionine. The target enzyme is G9a, and it selectively impairs G9a HMTase and the generation of H3K9me2 in vitro. BIX-01294 (4.1 μM) reduces H3K9me2 Levels in bulk histone preparations from wt ES cells, mouse embryonic fibroblasts and HeLa cells. BIX-01294 reduces H3K9me2 at Several G9a Target Genes including Bim1 and Serac1.
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Source | Cancer Cell Int (2015). Figure 1. BIX 01294 |
| Method | Western blot analysis | |
| Cell Lines | human bladder cancer cells | |
| Concentrations | 1.25, 2.5, 5, 10 and 20 μmol/l | |
| Incubation Time | 24 h | |
| Results | In summary, BIX-01294, as a specific inhibitor of EHMT2, induces caspase-dependent apoptosis in a dose- and time-dependent manner in human bladder cancer cells. |
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 cells |
| Preparation method | MCF-7 cells treated with 10 μM BIX were fixed in 4% glutaraldehyde. After dehydration, ultrathin sections were prepared using a Sorvall MT5000 microtome (DuPont Instruments, MT5000), and collected on 150 mesh copper grids. Sections were stained with 1% uranyl acetate and/or lead citrate, and images obtained with a JEOL 100CX transmission electron microscope (JEOL USA, JEOL-100CX). |
| Concentrations | 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6 mice |
| Formulation | |
| Dosages | 2 μl |
| Administration | injected through implanted cannula |
| Molecular Weight | 600.02 |
| Formula | C28H38N6O2.3HCl |
| CAS Number | 1392399-03-9 |
| Solubility (25°C) | DMSO 60 mg/mL Water 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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