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BIX-01294 trihydrochloride

Catalog No. T1959 CAS 1392399-03-9

Synonyms: BIX 01294

BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.

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BIX-01294 trihydrochloride Chemical Structure

BIX-01294 trihydrochloride, CAS 1392399-03-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 65.00
10 mg	In stock	$ 109.00
25 mg	In stock	$ 202.00
50 mg	In stock	$ 288.00
100 mg	In stock	$ 518.00
500 mg	In stock	$ 1,160.00
1 mL * 10 mM (in DMSO)	In stock	$ 142.00

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Purity: 99.95%

Purity: 98.98%

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Storage & Solubility Information

Description	BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
Targets&IC50	G9a:2.7 μM
In vivo	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).
Kinase Assay	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).

Synonyms	BIX 01294
Molecular Weight	600.02
Formula	C28H38N6O2·3HCl
CAS No.	1392399-03-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 60 mg/mL (100 mM)

DMSO: 60 mg/mL (100 mM)

References and Literature

1. Kubicek S, et al. Mol Cell, 2007, 25(3), 473-481. 2. Imai K, et al. J Biol Chem, 2010, 285(22), 16538-16545. 3. Zhang W, Yang D, Yuan Y, et al. Muscular G9a regulates muscle-liver-fat axis by musclin under overnutrition in female mice[J]. Diabetes. 2020 4. Zhang Y, Xue W, Zhang W, et al. Histone methyltransferase G9a protects against acute liver injury through GSTP1. Cell Death & Differentiation. 2019: 1-16. 5. Liu Shanshan, Yu Sun, Ming Jiang, Yangkai Li, Ye Tian, Weili Xue, Ninghe Ding, Zheng Ling, et al. Glyceraldehyde-3-phosphate dehydrogenase promotes liver tumorigenesis by modulating phosphoglycerate dehydrogenase [J]. Hepatology. 2017 Aug;66(2):631-645

Citations

1. Liu Shanshan, Yu Sun, Ming Jiang, Yangkai Li, Ye Tian, Weili Xue, Ninghe Ding, Zheng Ling, et al. Glyceraldehyde-3-phosphate dehydrogenase promotes liver tumorigenesis by modulating phosphoglycerate dehydrogenase. Hepatology. 2017 Aug;66(2):631-645 2. Zhang Y, Xue W, Zhang W, et al. Histone methyltransferase G9a protects against acute liver injury through GSTP1. Cell Death & Differentiation. 2020, 27(4): 1243-1258 3. Zhang W, Yang D, Yuan Y, et al. Muscular G9a regulates muscle-liver-fat axis by musclin under overnutrition in female mice. Diabetes. 2020

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Stem Cell Differentiation Compound Library Bioactive Compounds Library Max Methylation Compound Library Epigenetics Compound Library Anti-Cancer Compound Library Bioactive Compound Library Anti-COVID-19 Compound Library Chromatin Modification Compound Library

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Keywords

BIX-01294 trihydrochloride 1392399-03-9 Autophagy Chromatin/Epigenetic Histone Methyltransferase SUV39H1(H320R) p21 recurrent BIX-01294 Trihydrochloride Cdkn1a MLKL H3K9me3 inhibit PRMT1 p53 Inhibitor H3K9me2 BIX01294 BIX 01294 trihydrochloride BIX-01294 BIX 01294 Trihydrochloride BIX01294 Trihydrochloride BIX 01294 Gadd45a BIX01294 trihydrochloride inhibitor

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