JAK/STAT Signaling - JAK
The JAK (Janus kinase) / STAT (signal transducer and activator of transcription) signaling pathway transduce signals that are essential for development, cellular differentiation and homeostasis. This pathway plays a critical role in cytokine receptor systems, regulating growth, survival and pathogen resistance. JAK is a family of non-receptor protein tyrosine kinases, consisting of JAK1, JAK2, JAK3 and TYK2 (Tyrosine Kinase-2). STATs are transcription factors that activated following recruitment to an activated receptor complex, seven STAT proteins have been identified: STAT1, STAT2, STAT3, STAT4, STAT5A, STAT5B and STAT6.
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.
- B1130 GLPG06341 CitationTarget: JAKSummary: JAK1 inhibitor
- A4512 Cucurbitacin ITarget: STAT|JAKSummary: STAT3/JAK2 signaling inhibitor
- A4511 CercosporamideTarget: JAK|MNKSummary: Mnk2 and JAK3 inhibitor
- A3937 XL019Target: JAKSummary: JAK2 inhibitor,potent and selective
- A3741 Pyridone 6Target: JAKSummary: Pan-JAK inhibitor
- A4152 BMS-911543Target: JAKSummary: JAK2 inhibitor,selective small molecule
- A4151 ZM 39923 HClTarget: JAKSummary: JAK3 inhibitor,potent and selective
- A4150 WHI-P154Target: VEGFR|Src|EGFR|JAKSummary: JAK3 inhibitor
- A4149 S-Ruxolitinib (INCB018424)Target: JAKSummary: JAK1/2 inhibitor,potent and selective
- A4148 NVP-BSK805 2HClTarget: JAKSummary: JAK2 inhibitor