B9311
BIX 01294 trihydrochloride hydrate
≥98% (HPLC), powder
Sinónimos:
2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride hydrate
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About This Item
Fórmula empírica (notación de Hill):
C28H38N6O2·3HCl · xH2O
Número de CAS:
Peso molecular:
600.02 (anhydrous basis)
Código UNSPSC:
12352200
NACRES:
NA.77
Productos recomendados
Nivel de calidad
Ensayo
≥98% (HPLC)
Formulario
powder
condiciones de almacenamiento
desiccated
color
white
solubilidad
H2O: >20 mg/mL
temp. de almacenamiento
2-8°C
Descripción general
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.
Aplicación
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
Acciones bioquímicas o fisiológicas
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.
Características y beneficios
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.
Otras notas
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.
Código de clase de almacenamiento
11 - Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
Equipo de protección personal
Eyeshields, Gloves, type N95 (US)
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Journal of Alzheimer's disease : JAD, 70(4), 1175-1185 (2019-07-20)
Emerging evidence suggests that epigenetic dysregulation of gene expression is one of the key molecular mechanisms of neurodegeneration and Alzheimer's disease (AD). However, little is known about the role of epigenetic dysregulation on synaptic dysfunction in humans, because of the
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Nature biotechnology, 26(7), 795-797 (2008-06-24)
Reprogramming of mouse and human somatic cells can be achieved by ectopic expression of transcription factors, but with low efficiencies. We report that DNA methyltransferase and histone deacetylase (HDAC) inhibitors improve reprogramming efficiency. In particular, valproic acid (VPA), an HDAC
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Journal of neurovirology, 24(2), 192-203 (2017-12-20)
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Inhibition of H3K9 methyltransferase G9a repressed cell proliferation and induced autophagy in neuroblastoma cells
Ke XX, et al.
PLoS ONE, 9(9), e106962-e106962 (2014)
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Oncology letters, 15(6), 9757-9765 (2018-06-22)
Euchromatic histone-lysine N-methyltransferase (G9A), the primary histone methyltransferase for histone H3 Lys9, has been identified to be upregulated in numerous types of cancer. The aim of the present study was to analyze the clinical significance of G9A, and preliminarily explore
Artículos
Epigenetic modifications are thought to occur through two key interconnected processes—DNA methylation and the covalent modification of histones.
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