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Epigenetics

Epigenetics is one of the emerging fields which have the potential to explain mechanisms of aging, human development, the origins of cancer, heart disease, mental illness, as well as several other diseases. The molecular basis of epigenetics includes both DNA modification and Histone modification. Histone modification (particularly N-terminal of the histones) is the major process for regulating eukaryotic gene expression. It includes histone actylation, phosphorylation, methylation and ubiquitination. The combination of different histone modifications results in either active DNA conformation or repressive DNA conformation which subsequently leads to the activation or repression of certain gene expression. Overall, the property of epigenetic enzymes make them important targets in drug development.

HD Biosciences offers comprehensive epigenetic solutions and services from assay development to high throughput screening (HTS) for histone methyltrasnferase, histone demethylase, histone acetylase and histone deacetylase.

Histone Methylation:
Demethylase and Methyltransferase (HMT)
Assay Formats: Fluorescence, Radiometric, Absorbance etc.
Assay development includes enzyme kinetic analysis (i.e. Km determination for substrate), enzyme titration and assay validation
Figure 1: IC50 determination of demethylase A using its specific inhibitor.
The IC50 determination was performed according to the standard procedure. Curve fitting was performed using GraphPad Prism 5 software.
Histone Acetylation
Deacetylase (HDAC) and Acetyltransferase (HAT) biochemical assay
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Assay Formats: Caliper, HDAC-Glo, SIRT-Glo
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Assay development includes enzyme kinetic analysis (i.e. Km determination for substrate), enzyme titration and assay validation
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Available target:
HDAC1
HDAC3
HDAC6
HDAC8
SIRT1
SIRT2
SIRT3
Figure 2: IC50 determination of reference compounds against HDAC6 using Caliper Mobility Shift assay format
Figure 3: IC50 determination of reference compounds against HDAC8 using HDAC-Glo assay format
The IC50 determination was performed according to the standard procedure. Curve fitting was performed using GraphPad Prism 5 software
Deacetylase (HDAC) cell based assay
HDB provides unique HDAC cell based assay which is validated with reference compounds on Hela cell line.
Figure 4: IC50 determination of cell based HDAC's inhibition against reference compounds on Hela cell line.
The IC50 determination was performed according to the standard procedure. Curve fitting was performed using GraphPad Prism 5 software.
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HD Biosciences (China) Co.,Ltd
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Zhangjiang East Campus, Pudong, Shanghai 201201,
P.R.China
Tel: (+86) 21-51163700
Fax: (+86) 21-51163766
operation@hdbiosciences.com