Transcription is an important first step in the conversion of genetic information in the DNA into proteins, and is the main link in the control of gene expression. Transcription of protein-coding genes is accomplished by the multi-subunit enzyme RNA polymerase II and an ensemble of ancillary proteins which is called transcription factors (TFs). TFs play an important role in the long-term regulation of cell growth, differentiation and response to environmental signals. Recently, interest has focused on the study of small molecules targeting TFs, which contribute to the investigation of the pathogenesis of a wide range of human diseases, such as diabetes, inflammatory diseases and cardiovascular diseases. Therefore, these proteins have great therapeutic potential.
BOC Sciences has designed a dedicated set of more than 9,200 transcription-related screening compounds with validated transcription factor targets modulating properties for high-throughput screening. Our library of transcription factor targeted compounds is a useful tool for studying transcription factors as drug targets, and regulating TFs for different therapeutic applications.
Figure 1. Mechanisms of HIF Stabilization by Immune Cells (A) O2 dependent. (Palazon, A.; et al. 2014)
Library Design
- Firstly, a reference set of known modulators of transcription-associated proteins are obtained from a wide range of commercial databases
- Then, a 2D fingerprint similarity search is performed against the BOC Sciences HTS compound collection
- Nearly 23,700 transcription-related molecules are generated successfully
The search is performed against the following transcription-related protein targets:
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Transcription-related Screening Library Characteristics
- No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
- Bioactivity and safety confirmed by preclinical studies and clinical trials
- Structural diversity, medicinal activity, and cellular penetration
- Structural document, IC50, and other chemical and biological data are provided
- Tanimoto index ≥ 0.8
- All compounds are continually updated
- Compound cherry-picking service is provided
What We Deliver
- Delivered within 2 weeks in any customer-preferred format
- Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
- All compounds have a minimum purity of 90% assessed by 1H NMR and HPLC
- Analytical data is provided
BOC Sciences provides professional, rapid and high-quality services of Transcription-related Screening Library design at competitive prices for global customers. Personalized and customized services of Transcription-related Screening Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!
Reference
- Palazon, A.; et al. HIF Transcription Factors, Inflammation, and Immunity. Immunity. 2014. 41(4): 518-528.
