Phosphatidylinositol-4,5-bisphosphate 3-kinases (PI3K) δ and γ Subunits Inhibitors Library

Phosphatidylinositol-4,5-bisphosphate 3-kinases (also known as phosphatidylinositol 3-kinase) are a family of enzymes involved in several signaling cascade responses for cell growth, survival, proliferation, motility and morphology. A disorder of each of the pathways may contribute to the development of cancer. Elevated PI3K kinase activity is commonly associated with multiple cancers. PI3K can be classified into 3 classes, with different structures and functions. The most widely studied is Class IA PI3K with four types of catalytic subunits, namely p110α, β, δ, and γ. PI3K is involved in various immune responses, and is produced in different immune cells. p110α and p110β proteins are commonly expressed, and the p110δ and p110γ isoforms of PI3K have specific roles in the regulation of multiple aspects of immune defense and inflammation.

BOC Sciences has developed a library to provide potential small-molecule inhibitors of δ, and γ isoforms of PI3K.

Figure 1. The class I PI3K family. (Akinleye, A.; et al. 2013)

Library Design

At BOC Sciences, our PI3K δ and γ subunits inhibitors library is designed based on pharmacophore approach

• Firstly, we have collected crystallographic structures of validated PI3K α and β subunits from a variety of commercial databases
• Then, the most critical ligand-protein interactions are identified based on crystallography data and spatial alignments
• In this step, data on these pharmacophore sites are determined to prepare an in silico screening model
• Finally, we propose the library to generate potential small molecule inhibitors of the γ and δ isoforms of PI3K from class IA

PI3K δ and γ Subunits Inhibitors Library Characteristics

• 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. Schematic representation of the PI3K signaling pathway. (Akinleye, A.; et al. 2013)

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 Phosphatidylinositol-4,5-bisphosphate 3-kinases (PI3K) δ and γ Subunits Inhibitors Library design at competitive prices for global customers. Personalized and customized services of Phosphatidylinositol-4,5-bisphosphate 3-kinases (PI3K) δ and γ Subunits Inhibitors 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!