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.
-   A4193 SMI-4aTarget: PimSummary: Potent Pim inhibitor A4193 SMI-4aTarget: PimSummary: Potent Pim inhibitor
-   A3514 JAK2 Inhibitor V, Z3Summary: Jak2 tyrosine kinase inhibitor A3514 JAK2 Inhibitor V, Z3Summary: Jak2 tyrosine kinase inhibitor
-   A1835 Pelitinib (EKB-569)Summary: EGFR inhibitor,potent and irreversible A1835 Pelitinib (EKB-569)Summary: EGFR inhibitor,potent and irreversible
-   A4192 SGI-1776 free base3 CitationSummary: Pim kinase inhibitor,ATP-competitive A4192 SGI-1776 free base3 CitationSummary: Pim kinase inhibitor,ATP-competitive
-   A3339 CYT387 sulfate saltSummary: JAK1/JAK2 inhibitor A3339 CYT387 sulfate saltSummary: JAK1/JAK2 inhibitor
-   A1393 WZ8040Target: EGFRSummary: EGFR T790M inhibitor,irreversible amd potent A1393 WZ8040Target: EGFRSummary: EGFR T790M inhibitor,irreversible amd potent
-   A3962 AZD1208Target: PimSummary: PIM kinase inhibitor A3962 AZD1208Target: PimSummary: PIM kinase inhibitor
-   A3222 Baricitinib phosphateSummary: JAK1/JAK2 inhibitor A3222 Baricitinib phosphateSummary: JAK1/JAK2 inhibitor
-   A1389 WZ4002Summary: Mutant-selective EGFR inhibitor(L858R,T790M), irreversible and potent A1389 WZ4002Summary: Mutant-selective EGFR inhibitor(L858R,T790M), irreversible and potent
-   A3221 Bardoxolone methylTarget: Nrf2Summary: IKK inhibitor, potent antioxidant inflammation modulator A3221 Bardoxolone methylTarget: Nrf2Summary: IKK inhibitor, potent antioxidant inflammation modulator
