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.
Cell Experiment | |
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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 | |
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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 |
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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