Kinase Focused Library

Kinase is an enzyme that adds phosphate groups to substrate molecules, and this process is known as phosphorylation. Protein phosphorylation plays an important role in regulating a large number of cellular processes such as cell division, metabolism, and signal transduction, and 50% of cellular functions in the human genome are regulated by kinases. Kinases therefore are essential in new drug development, and protein kinases are one of the most promising drug targets in anticancer drug development. Many protein kinases are encoded in the human genome, and kinase inhibitors are an important class of drugs that block the activity of certain disease-related enzymes, such as cancer and inflammation. Although there are many reported kinase modulators, most of them share similar structural and selective issues.

BOC Sciences provides its unique protein kinase focused library, which contains approximately 32,000 drug-like screening compounds selected by ligand-based methods.

Figure 1. Processes leading to dissociation of the intramolecular inhibitory interaction in PKC and to activation of the enzyme. (Mochly-Rosen, D.; et al. 2012)

Library Design

1. Firstly, a reference set containing more than 135,000 compounds with reported kinase inhibitory activity (IC₅₀, Ki et al.; <10 μM, inhibition>50%) is extracted from a database with reliable sources
2. Then, we perform a a 2D fingerprint similarity search against the reference set of protein kinase activity modulators to analyze the the BOC Sciences HTS compound collection
3. Finally, the resulting screened compounds will be further filtered through an internal filter to remove PAINS, toxic substances and reactive fractions

Our well-designed kinase focused library contains analogs of kinase inhibitors against the following molecular targets:

Figure 2. Domain composition of PKC family members. (Mochly-Rosen, D.; et al. 2012)

Kinase Focused Library Characteristics

• No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
• Confirmed bioactivity and safety by preclinical studies and clinical trials
• Targets involved PI3K, HDAC, mTOR, CDK, JAK and other cancer-related targets
• Structural diversity, significant efficacy, and cellular penetration
• Structural document, IC₅₀, and other chemical and biological data are provided
• Tanimoto index ≥ 0.85
• 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 Kinase Focused Library design at competitive prices for global customers. Personalized and customized services of Kinase Focused 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!