Janus Kinase (JAK) Targeted Library

As one of non-receptor tyrosine kinase families, the Janus kinase (Jak) family is composed of four members, Jak1, Jak2, Jak3 and Tyrosine kinase 2 (Tyk2). Each protein has a similar protein structural domain structure: a kinase domain and a catalytically inactive pseudo-kinase domain, and each of them binds to a cytokine receptor via an amino-terminal structural domain. Jaks is able to be activated and phosphorylate the receptor upon binding of a cytokine to its receptor, creating docking sites for signaling molecules. Deficiency of JAK3 often leads to human autosomal recessive severe combined immunodeficiency (SCID), therefore, the development of a selective Jak3 inhibitor has promising therapeutic applications in the treatment of cancer and inflammatory diseases.

BOC Sciences can establish a Janus Kinase (JAK) targeted library that contains 600 molecules.

Figure 1. Principal signaling pathways activated by homodimeric cytokine receptors. (Vainchenker, W.; et al. 2018)

Library Design

1. Firstly, we collect and establish a reference set of known JAK1, JAK2 and JAK3 inhibitors from various databases
2. We employ advanced docking tools to identify some crucial amino acid residues involved in inhibitor binding
3. Then, our experts prepare three different binding models using a variety of screening tools based on accurate protein-ligand interaction data
4. Finally, the entire BOC Sciences compound collection is processed using multiple in-house filters to detect and remove PANS compounds

Figure 2. The kinase domain of Janus kinase 2 (JAK2). (Vainchenker, W.; et al. 2018)

Janus Kinase (JAK) Targeted 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

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 Janus Kinase (JAK) Targeted Library design at competitive prices for global customers. Personalized and customized services of Janus Kinase (JAK) Targeted 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!