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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Epigenetics>Histone Methyltransferase Inhibitors>BIX-01294 trihydrochloride
BIX-01294 trihydrochloride
  • BIX-01294 trihydrochloride

BIX-01294 trihydrochloride NEW

Price $37 $50 $65
Package 1mg 2mg 5mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-17

Product Details

Product Name: BIX-01294 trihydrochloride CAS No.: 1392399-03-9
Purity: 99.95% Supply Ability: 10g
Release date: 2024/11/17

Product Introduction

Bioactivity

名稱BIX-01294 trihydrochloride
描述BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
激酶實驗ATR for use in the in vitro enzyme assay is obtained from HeLa nuclear extract by immunoprecipitation with rabbit polyclonal antiserum raised to amino acids 400-480 of ATR contained in the following buffer: 25 mM HEPES (pH 7.4), 2 mM MgCl2, 250 mM NaCl, 0.5 mM EDTA, 0.1 mM Na3VO4, 10% v/v glycerol, and 0.01% v/v Tween 20. ATR-antibody complexes are isolated from nuclear extract by incubating with protein A-Sepharose beads for 1 h and then through centrifugation to recover the beads. In the well of a 96-well plate, 10 μL ATR-containing Sepharose beads are incubated with 1 μg of substrate glutathione?S-transferase-p53N66 (NH2-terminal 66 amino acids of p53 fused to glutathione?S-transferase are expressed in?E. coli) in ATR assay buffer (50 mM HEPES (pH 7.4), 150 mM NaCl, 6 mM MgCl2, 4 mM MnCl2, 0.1 mM Na3VO4, 0.1 mM DTT, and 10% (v/v) glycerol) at 37°C in the presence or absence of inhibitor. After 10 min with gentle shaking, ATP is added to a final concentration of 3 μM and the reaction continued at 37°C for an additional 1 h. The reaction is stopped by addition of 100 μL of PBS, and the reaction is transferred to a white opaque glutathione coated 96-well plate and incubated overnight at 4°C. This plate is then washed with PBS/0.05% (v/v) Tween 20, blotted dry, and analyzed by a standard ELISA technique with a phosphoserine 15 p53 antibody. The detection of phosphorylated glutathione?S-transferase-p53N66 substrate is performed in combination with a goat anti-mouse horseradish peroxidase-conjugated secondary antibody. Enhanced chemiluminescence solution is used to produce a signal, and chemiluminescent detection is carried out via a TopCount plate reader. The resulting calculated % enzyme activity is then used to determine the IC50?values for the compounds (IC50?taken as the concentration at which 50% of the enzyme activity is inhibited).
體內(nèi)活性In wild-type embryonic stem (ES) cells, mouse embryonic fibroblasts, and HeLa cells, BIX-01294 (4.1 μM) reduces the levels of H3K9me2. BIX-01294 can specifically inhibit G9a (IC50=1.7 μM) and GLP (IC50=38 μM).
存儲條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : 60 mg/mL (100 mM)
DMSO : 40 mg/mL (66.66 mM), Sonication is recommended.
關(guān)鍵字SUV39H1(H320R) | BIX-01294 trihydrochloride | p21 | recurrent | BIX-01294 Trihydrochloride | Cdkn1a | MLKL | H3K9me3 | inhibit | Histone Methyltransferase | PRMT1 | p53 | Autophagy | Inhibitor | H3K9me2 | BIX01294 | BIX 01294 trihydrochloride | BIX-01294 | BIX 01294 Trihydrochloride | BIX01294 Trihydrochloride | Gadd45a | BIX01294 trihydrochloride
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Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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