JAK/STAT Signaling

Various ligands including cytokines (e.g. interferons and interleukins), hormones (e.g. erythropoietin and growth hormone) and their cell surface receptors activate JAK proteins, which autophosphorylate, and then phosphorylate the receptor. Subsequently, JAKs phosphorylate a specific tyrosine residue on the STAT protein, promoting dimerization via SH2 domains. The activated STATs form homo-/heterodimers and translocate to the nucleus to trigger target gene transcription. In addition, suppressors of cytokine signaling (SOCS) family inhibit receptor signaling via homologous or heterologous feedback regulation. Dysregulation in JAK/STAT signaling is associated with diseases such as atherosclerosis, immunodeficiencies and cancer.
-   A3556 LKB1 (AAK1 dual inhibitor)Target: PimSummary: Pim-1 kinase inhibitor A3556 LKB1 (AAK1 dual inhibitor)Target: PimSummary: Pim-1 kinase inhibitor
-   A1367 ALK-IN-1Summary: Anaplastic lymphoma kinase (ALK) inhibitor A1367 ALK-IN-1Summary: Anaplastic lymphoma kinase (ALK) inhibitor
-   A2224 Stattic5 CitationTarget: STATSummary: STAT3 inhibitor,small-molecule and potent A2224 Stattic5 CitationTarget: STATSummary: STAT3 inhibitor,small-molecule and potent
-   C4533 RO8191Summary: IFN-α receptor 2 agonist C4533 RO8191Summary: IFN-α receptor 2 agonist
-   A3012 Ruxolitinib (INCB018424)4 CitationTarget: JAKSummary: JAK1 and JAK2 inhibitor A3012 Ruxolitinib (INCB018424)4 CitationTarget: JAKSummary: JAK1 and JAK2 inhibitor
-   A3337 CX-6258Summary: Pan-Pim kinases Inhibitor A3337 CX-6258Summary: Pan-Pim kinases Inhibitor
-   A1173 AG-18Summary: EGFR/PDGFR inhibitor A1173 AG-18Summary: EGFR/PDGFR inhibitor
