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.
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A4151 ZM 39923 HClTarget: JAKSummary: JAK3 inhibitor,potent and selective -
A8319 Dacomitinib (PF299804, PF299)Target: ErbBSummary: HER inhibitor -
A4150 WHI-P154Target: VEGFR|Src|EGFR|JAKSummary: JAK3 inhibitor -
A8247 Afatinib (BIBW2992)1 CitationTarget: EGFRSummary: Irreversible EGFR/HER2 inhibitor -
A4149 S-Ruxolitinib (INCB018424)Target: JAKSummary: JAK1/2 inhibitor,potent and selective -
A8234 Erlotinib Hydrochloride2 CitationSummary: Selective EGFR inhibitor -
A4148 NVP-BSK805 2HClTarget: JAKSummary: JAK2 inhibitor -
A8219 Gefitinib (ZD1839)15 CitationTarget: EGFRSummary: Selective EGFR inhibitor -
A4147 LY2784544Target: Aurora Kinases|FLT3|VEGFR|FGFR|Trk Receptors|JAK|ALK|TYK2|MUSK|MAP3KSummary: JAK2 inhibitor,highly potent and selective -
A8218 Lapatinib7 CitationTarget: ErbBSummary: EGFR/HER2 inhibitor,potent,selective and reversible
