QL-1200186 is a selective, orally active, allosteric inhibitor targeting the tyrosine kinase TYK2 pseudokinase domain JH2 ( IC 50 =0.06 nM, TYK2 JH2 ), with 164-fold selectivity over TYK1 JH2 ( IC 50 =9.85 nM, TYK1 JH2 ). QL-1200186 first stabilizes the TYK2 JH2 conformation, inhibits the activity of the JH1 catalytic domain, and blocks the IFNα , IL-12/IL-23 -mediated JAK-STAT signaling pathway. QL-1200186 can inhibit the production of Th1/Th17 cell-related cytokines (such as IFNγ , IL-23 ), reduce immune cell activation, and has no significant effect on JAK1/2/3 kinase activity. QL-1200186 can significantly improve skin inflammation in the Imiquimod ( HY-B0180 )-induced psoriasis mouse model and reduce the Psoriasis Area and Severity Index (PASI) score. QL-1200186 can be used in the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE).
Products | Products > Disease Areas > Inflammation or Immune System Disease | Products > Signaling Pathways > JAK/STAT Signaling | Products > Signaling Pathways > Stem Cell/Wnt | Products > Signaling Pathways > Immunology/Inflammation | Products > Research Areas > Inflammation/Immunology | Products > Signaling Pathways > STAT | Products > Signaling Pathways > Interleukin Related | Products > Signaling Pathways > IFNAR
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