B9311
BIX 01294 trihydrochloride hydrate
≥98% (HPLC), powder
Synonym(s):
2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride hydrate, BIX 01294
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About This Item
Empirical Formula (Hill Notation):
C28H38N6O2·3HCl · xH2O
CAS Number:
Molecular Weight:
600.02 (anhydrous basis)
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white
solubility
H2O: >20 mg/mL
storage temp.
2-8°C
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.
Application
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
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.
Features and Benefits
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
Other Notes
BIX-01294 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the BIX-01294 probe summary on the Chemical Probes Portal website.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Personal Protective Equipment
dust mask type N95 (US), Eyeshields, Gloves
Certificates of Analysis (COA)
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Articles
Epigenetic modifications are thought to occur through two key interconnected processes—DNA methylation and the covalent modification of histones.
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