Proline Kinase Library

Name: Proline Kinase Library
Brand: BOC Sciences

Protein kinases are usually classified as serine/threonine or tyrosine kinases, with the serine or threonine residues preceding proline (Ser/Thr-Pro) being the main regulatory phosphorylation motifs that play a role in various cellular processes. Proline-directed kinases such as the mitogen-activated protein (MAP) kinase, cyclin-dependent protein kinase 5 (CDK5) and glycogen synthase 3 (GSK3) of the tau protein are associated closely with many human diseases. These kinases and phosphatases play critical roles in various cellular processes such as the cell cycle, transcription and various signal-transduction pathways, as well as in the cancer and Alzheimer's disease. Scientists are investigating proline-directed kinase-dependent pathways to identify rational targets for the therapeutic intervention of Alzheimer's disease and other neurological disorders.

BOC Sciences builds a proline kinase library which contains 2,000 compounds.

Figure 1. DFG-out conformation in PYK2. (Han, S.; et al. 2009)

Library Design

At BOC Sciences, a proline kinase library is designed and constructed by employing the CADD approach based on the corresponding characteristics of proline kinase.

Kinases

ERKs
CDKs
GSK
JNK
MAP and related signaling MAPKAPKS

2D structural similarity (Tanimoto) and topological pharmacophores

Cluster: 730
Number of screens: 6668
Common diversity: 0.74
Singeltones: 215

Proline Kinase Library Characteristics

We provide multiple topological analogues
Representative examples of compounds with max, diversity of 1% random selection are available
Favorable physicochemical parameters and solubility requirements
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
All compounds are continually updated
Compound cherry-picking service is provided

Figure 2. Active site structure of PYK2 in complex with PF-4618433. (Han, S.; et al. 2009)

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 Proline Kinase Library design at competitive prices for global customers. Personalized and customized services of Proline Kinase 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

Han, S.; et al. Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design. Journal of Biological Chemistry. 2009. 284(19): 13193-13201.

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Services Based on the Chemical Library Design Platform

BOC Sciences has rich experience in working with global customers in custom library synthesis of compounds and generating small to medium-sized libraries of target compounds. Our knowledge in generating a large number of target molecules in a remarkably shorter time enables quick biological screenings for affinities. With the target properties in mind, we deliver target molecules, by applying our extensive knowledge in drug discovery.

Our mission is to provide clients with a professional chemical library design platform. Empowered by high-quality services and effective research solutions, we are committed to helping customers achieve effective and successful research goals.