JAK-STAT信号配体
The chemical signals outside of the cell to the cell nucleus are transferred by JAK-STAT signaling pathways. These pathways are involved in cell division and death, processes of the immune response, etc. Initially, the dimerization of the extracellular domains of receptor Janus kinase(JAK) brings together the intracellular domains of protein induced by ligand binding(cytokine, for example). The JAKs phosphorylate each other, resulting in the activation of the kinases. The activated JAKs can phosphorylate a regulator of gene expression called STAT(Signal Transducer and Activator of Transcription). Activated STAT moves to the nucleus to regulate gene expression. Any deviations during JAK-STAT signaling pathways may lead to cancer, serious skin diseases, or immune system disorders. Thus, investigation in this area is one of the valuable targets for drug discovery.
JAK-STAT Signaling Ligands Library contains 384 small ligands, some representative molecules are given below: Pazopanib, VEGFR receptor inhibitor; LY294002, TPK inhibitor; PF06700841, JAK1 inhibitor; SH-4-54, STAT3 inhibitor.
Related terms: epidermal growth factor, Janus kinase, platelet derived growth factor, Pim-1 proto-oncogene, serine/threonine kinase, colony stimulating factor, interleukin
JAK-STAT signaling pathway(Created by BioRender.com)
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Highlights
Pazopanib, VEGF receptor inhibitor
LY294002, Tyrosine-protein kinases inhibitor
PF-06700841, JAK1 inhibitor
SH-4-54, STAT3 inhibitor
Product Features
A set of 384 JAK-STAT signaling relevant molecules with sub-10 micromolar activity coefficient values for HTS/HCS programs.
The library is composed of ligands that target all major pharmaceutically relevant GPCR targets.
JAK-STAT Signaling Ligands Library covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
Calculated structural diversity of the collection: 0.86.
Comprehensive documentation with structures, trivial names, synonyms, activity coefficients values, types of action on target and references to original literature.
NMR and LCMS validated purity.
All the compounds are available in stock for hit follow-up.
The library is continuously updated.
Product Details
Format: 10 - 100 µL of 10 mM DMSO stock solutions; dry powders (1 mg);
Container: 384-well microplates;
Storage: - 18 °C;
Shipping: Dry ice.
Utility
High throughput screening (HTS);
High content screening (HCS);
Cherry picking.
