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BIX 01294 Trihydrochloride

Cat. No. M2024
BIX 01294 Trihydrochloride Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 150  USD150 In stock
10mg USD 125  USD125 In stock
50mg USD 380  USD380 In stock
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Quality Control & Documentation
Biological Activity

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.

Customer Product Validations & Biological Datas
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.
Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Upadhyay AK, et al. J Mol Biol. An analog of BIX-01294 selectively inhibits a family of histone H3 lysine 9 Jumonji demethylases.

[2] Chang Y, et al. Nat Struct Mol Biol. Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294.

[3] Kubicek S, et al. Mol Cell. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.

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Keywords: BIX 01294 Trihydrochloride supplier, Histone Methyltransferase, inhibitors, activators


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