Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and JAK1 and JAK2 stimulates IFN-gamma. JAK Inhibitor I is a pyridine-containing...

Soluble in DMSO. Merck 5, also known as Pyridone 6, is a potent and reversible ATP-competitive inhibitor of the JAK kinases (JAK1, JAK2, JAK3, and Tyk2) with IC(50) values in the low anomolar range. At higher values (IC(50) >100nM) Merck 5 also can inhibit ERK kinase family and appear to block IL-2 and IL-4...