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.
-
A8779 WM-80141 CitationSummary: Inhibitor for KAT6A (MOZ) and KAT6B (MORF/QKF), anticancer -
A8218 Lapatinib7 CitationTarget: ErbBSummary: EGFR/HER2 inhibitor,potent,selective and reversible -
A8197 Compound 561 CitationTarget: EGFRSummary: REGFR inhibitor -
A8199 PD153035 hydrochloride1 CitationTarget: EGFRSummary: Potent EGFR inhibitor -
A3012 Ruxolitinib (INCB018424)12 CitationTarget: JAKSummary: JAK1 and JAK2 inhibitor -
A4092 CUDC-1011 CitationTarget: Histone Deacetylases (HDACs)|EGFR|ErbBSummary: Multitargeted HDAC inhibitor -
A4135 Tofacitinib (CP-690550) Citrate6 CitationTarget: JAKSummary: Potent JAK inhibitor -
A4136 TG101348 (SAR302503)2 CitationTarget: FLT3|JAK|c-RETSummary: JAK-2 inhibitor,potent and selective -
A4137 AZD1480Target: JAKSummary: JAK2 inhibitor,ATP-competitive and novel -
A4138 Tofacitinib (CP-690550,Tasocitinib)1 CitationTarget: JAKSummary: Janus kinase inhibitor

