Protein-tyrosine Phosphatase 1B (PTP1B) Inhibitors Library

Protein tyrosine phosphatase 1B is an important therapeutic target for several human diseases, including type 2 diabetes, obesity and cancer. A large number of molecules of broad chemical diversity have been reported as potent and selective PTP1B inhibitors that are superior to other protein tyrosine phosphatases. Some of these molecules have shown their potential to treat a variety of human diseases in various animal models, but only a very limited number of PTP1B inhibitors have entered clinical trials. Therefore, the development of potent, highly selective and safe PTP1B inhibitors remains imperative and important.

BOC Sciences has developed a library to provide potential small-molecule inhibitors of PTP1B.

Figure 1. Binding mode of compounds 1, 2 and 3 in PTP1B. (Akinleye, A.; et al. 2013)

Library Design

• Since PTP1B has a specific active site, we have focused on the selectivity of PTP1B inhibitors
• BOC Sciences has developed two binding models based on crystal structures and interaction maps to fully cover the prospective chemical space
• Both screening models are well validated using a set of potent reference compounds

PTP1B 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. Two dimensional maps of interaction from the complexes PTP1B-1. (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 Protein-tyrosine Phosphatase 1B (PTP1B) Inhibitors Library design at competitive prices for global customers. Personalized and customized services of Protein-tyrosine Phosphatase 1B (PTP1B) 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!