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BIX 01294 Trihydrochloride

Cat. No. M2024
BIX 01294 Trihydrochloride Structure
Size Price Availability Quantity
10mM/1mL In DMSO USD 150 In stock
10mg USD 120 In stock
50mg USD 380 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 600.02
Formula C28H38N6O2.3HCl
CAS Number 1392399-03-9
Purity >98%
Solubility DMSO 90 mg/mL
Water 90 mg/mL
Storage at -20°C
References

An analog of BIX-01294 selectively inhibits a family of histone H3 lysine 9 Jumonji demethylases.
Upadhyay AK, et al. J Mol Biol. 2012 Feb 24;416(3):319-27. PMID: 22227394.

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294.
Chang Y, et al. Nat Struct Mol Biol. 2009 Mar;16(3):312-7. PMID: 19219047.

Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.
Kubicek S, et al. Mol Cell. 2007 Feb 9;25(3):473-81. PMID: 17289593.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BIX 01294 Trihydrochloride supplier, Histone Methyltransferase, inhibitors

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