1392399-03-9

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 NO: 1392399-03-9
• Molecular Formula: C28H41Cl3N6O2
• Molecular Weight: 600.02314
• Product Categories: Inhibitors
• Mol File: 1392399-03-9.mol
• Article Data: 0

Chemical Properties

• Appearance: white/
• Storage Temp.: 2-8°C
• Solubility: H2O: >20mg/mL
• CAS DataBase Reference: BIX 01294(CAS DataBase Reference)
• NIST Chemistry Reference: BIX 01294(1392399-03-9)
• EPA Substance Registry System: BIX 01294(1392399-03-9)

Safety Data

• WGK Germany: 3
• Hazardous Substances Data: 1392399-03-9(Hazardous Substances Data)

Usage

Description

BIX 01294, also known as BIX 01294 trihydrochloride hydrate, is a diazepin-quinazolinamine derivative that functions as a histone-lysine methyltransferase (HMTase) inhibitor. It modulates the epigenetic status of chromatin by inhibiting the G9aHMTase dependent levels of histone-3 lysine (9) methylation (H3K9me). BIX 01294 has potential applications in various fields, including cancer research and stem cell induction.

Uses

Used in Cancer Research:
BIX 01294 is used as a histone methylation inhibitor for analyzing green fluorescent protein (d2EGFP) expression in E4 cells. It is also utilized to investigate the role of G9a in neuroblastoma tumor growth and as a specific inhibitor of G9a to treat various neuroblastoma cell lines, such as SK-N-AS, BE(2)-C, SK-N-DZ, SK-N-F1, and SHEP1.
Used in Stem Cell Induction:
In the field of stem cell research, BIX 01294 is used in combination with valproic acid, a histone deacetylase (HDAC) inhibitor, to potentially replace the requirement for ectopic OCT4 (POU5F1) and cMyc in pluripotent stem cell induction (iPS) recipes. This application highlights its potential in advancing the understanding and development of induced pluripotent stem cells for regenerative medicine and other therapeutic applications.

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.