Spleen Tyrosine Kinase (SYK) Inhibitors Library

Splenic tyrosine kinase is a non-receptor tyrosine kinase, and is important for downstream signaling from several cell surface receptors. SYK is able to bind B-cell receptor (BCR) activation with downstream signaling pathways that affect cell survival and proliferation. In addition, SYK can have either oncogenic or tumor suppressor activity in human malignancies. Due to its overexpression in hematopoietic cells, SYK is considered as a pro-survival factor for several hematological and non-hematological cancers. Nowadays, SYK kinase is a promising therapeutic target for diseases such as arthritis, allergic diseases, idiopathic thrombocytopenic purpura, systemic lupus erythematosus, and B-cell lymphoma. In addition, recent studies suggest that SYK inhibition may have antileukemic effects in human acute myeloid leukemia (AML).

BOC Sciences has established a library of SYK inhibitors, providing an opportunity to use small-molecule inhibitors of SYK for the treatment of immune diseases and cancer.

Figure 1. Spleen tyrosine kinase (Syk)-mediated signaling in B-cell receptor (BCR) and T-cell receptor (TCR). (Pamuk, O. N.; Tsokos, G. C. 2010)

Library Design

At BOC Sciences, our teams have employed an in silico screening strategy based on molecular docking method to generate this library which contains novel chemical structures with well-predicted affinity to the active site

1. A receptor-based virtual screening process is created based on X-ray data for the complexes
2. The compounds in the HTS compound collection have been pre-filtered using BOC Sciences' internal filters and then docked at the active site
3. Then, an interaction map of the known SYK inhibitor and one of the screened compounds in the active site of the kinase (PDBID: 4XG9) are generated
4. Finally, potential SYK inhibitors selected with computational chemistry, and virtual screening techniques are generated successfully

SYK 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. Selective oral spleen tyrosine kinase inhibitor. (Lamb,. D.; et al. 2016)

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 Spleen Tyrosine Kinase (SYK) Inhibitors Library design at competitive prices for global customers. Personalized and customized services of Spleen Tyrosine Kinase (SYK) 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!