BIX 01294

BIX 01294 Basic information
Product Name:BIX 01294
Synonyms:BIX 01294 Trihydrochloride Hydrate;4-Quinazolinamine, 2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-, hydrochloride (1:3);2-(Hexahydro-4-Methyl-1H-1,4-Diazepin-1-yl)-6,7-Dimethoxy-[1-(Phenylmethyl)-4-Piperidynyl]-4-Quinazolinamine Trihydrochloride BIX01294 hydrochloride;BIX01294 hydrochloride;BIX01294 3hydrochloride;Trihydrochloride Hydrate;N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine;BIX 01204
CAS:1392399-03-9
MF:C28H41Cl3N6O2
MW:600.02314
EINECS:
Product Categories:Inhibitors
Mol File:1392399-03-9.mol
BIX 01294 Structure
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
MSDS Information
BIX 01294 Usage And Synthesis
UsesBIX 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 DescriptionBIX-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 ActionsBIX 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.
storageroom temperature (desiccate)
BIX 01294 Preparation Products And Raw materials
OG-L002 MM-102 (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol GSK 343 GSK J4 HCl Tazemetostat (EPZ-6438)

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