Sphingosine-1-phosphate Lyase (SPL1) Inhibitors Library

Sphingosine-1-phosphate lyase, a polar sphingolipid metabolite, cleaves phosphorylated sphingosine bases (PSBs) into fatty aldehydes and phosphoethanolamine. SIP is capable of regulating various process such as cell migration, differentiation, survival, and complex physiological processes. S1P functions primarily through the activation of a subgroup of the endothelial differentiation gene (EDG) family of G protein-coupled cell surface receptors. The biological effects of S1P receptor signaling involve multiple pathways, including mitogen-activated protein kinase (MAPK), c-Jun N-terminal kinase (JNK), extracellular-signal-regulated kinase (ERK), phosphatidylinositol 3-kinase (PI3K), phospholipase C, phospholipase D, and other downstream mediators. SPL is expressed in many mammalian tissues, with typically low tissue levels of S1P. Therefore, inhibitors of SPL may be effective therapeutic agents for a variety of diseases involving S1P.

Figure 1. Sphingosine-1-phosphate signaling pathway. (González-Fernández, B.; et al. 2017)

Library Design

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

1. Firstly, we apply the crystal structure of the ligand and its interaction map
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. Finally, our experts produce a SPL1 inhibitors library comprising compounds with excellent 3D pharmacophore matching

SPL1 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. Regulation of sphingosine-1-phosphate signaling pathway in hepatic stellate cells (HSCs). (González-Fernández, B.; et al. 2017)

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 Sphingosine-1-phosphate Lyase (SPL1) Inhibitors Library design at competitive prices for global customers. Personalized and customized services of Sphingosine-1-phosphate Lyase (SPL1) 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!