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.
- A4139 AG-4903 CitationTarget: EGFR|JAKSummary: JAK2/EGFR inhibitor
- A4140 WP1066Target: STAT|JAKSummary: JAK2/STAT3 inhibitor,cell-permeable
- A4141 Baricitinib (LY3009104, INCB028050)2 CitationSummary: JAK1/JAK2 inhibitor,selective orally bioavailable
- A4143 CYT3871 CitationSummary: JAK-1/-2 inhibitor,ATP competitive
- A4144 AZ 960Target: JAKSummary: JAKs inhibitor
- A4145 TG101209Summary: JAK2/3 inhibitor
- A4146 CEP-337791 CitationSummary: JAK2 inhibitor,highly selective
- A4147 LY2784544Target: Aurora Kinases|FLT3|VEGFR|FGFR|Trk Receptors|JAK|ALK|TYK2|MUSK|MAP3KSummary: JAK2 inhibitor,highly potent and selective
- A4148 NVP-BSK805 2HClTarget: JAKSummary: JAK2 inhibitor
- A4149 S-Ruxolitinib (INCB018424)Target: JAKSummary: JAK1/2 inhibitor,potent and selective