BIX 01294 Chemical Properties

storage temp. 

Inert atmosphere,2-8°C

solubility 

H2O: >20mg/mL

form 

powder

color 

white

Safety Information

WGK Germany 

3

HS Code 

2933.99.8290

BIX 01294 Usage And Synthesis

Uses

BIX 01294 trihydrochloride hydrate has been used:

• as a histone methylation inhibitor to treat E4 cells for analysing green fluorescent protein (d2EGFP) expression
• to investigate the role of G9a in neuroblastoma tumor growth
• as specific inhibitor of G9a to treat the SK-N-AS, BE(2)-C, SK-N-DZ, SK-N-F1, and SHEP1 neuroblastoma cell lines

General Description

BIX-01294, a diazepin-quinazolinamine derivative, is a histone-lysine methyltransferase (HMTase) inhibitor that modulates the epigenetic status of chromatin. BIX-01294 inhibits the G9aHMTase dependent levels of histone-3 lysine (9) methylation (H3K9me). Bix-01294 and valproic acid, a histone deacetylase (HDAC) inhibitor, may replace the requirement for ectopic OCT4 (POU5F1) and cMyc respectively in pluripotent stem cell induction (iPS) recipes.

Biochem/physiol Actions

BIX 01294 is a selective histone methyl transferase inhibitor. 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.

storage

room temperature (desiccate)

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