JAK3-IN-6

Description: JAK3-IN-6 is a novel potent, selective, and irreversible inhibitor of Janus Associated Kinase 3 (JAK3) with an IC50 of 0.15 nM. JAK3-IN-6 was 4300-fold selective for JAK3 over JAK1 in enzyme assays, 67-fold interleukin (IL)-2 versus IL-6 or 140-fold IL-2 versus erythropoietin or granulocyte-macrophage colony-stimulating factor (GMCSF) selective in cellular reporter assays and > 35-fold selective in human peripheral blood mononuclear cell assays (IL-7 versus IL-6 or GMCSF). In vivo, selective JAK3 inhibition was sufficient to block the development of inflammation in a rat model of rheumatoid arthritis, while sparing hematopoiesis.

References: J Pharmacol Exp Ther. 2017 May; 361(2):229-244.