JAK3-IN-6

Biological Activity

JAK3-IN-6 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM and 740 nM for JAK3, JAK1 and JAK2, respectively. It is more selective for JAK3 than BMX, EGFR, ITK and BTK.

in vitro

JAK3-IN-6 is a potent JAK3 inhibitor with IC50 of 0.15 nM, with 4300-fold selectivity for JAK3 over JAK1 in enzymatic activity assays, erythropoietin and 67-fold and 140-fold higher selectivity for granulocyte-macrophage colony-stimulating factor.

in vivo

JAK3-IN-6 completely inhibits the progression of inflammatory responses.

target

Target	Value
JAK3 (Cell-free assay)	0.07 nM(Ki)
JAK1 (Cell-free assay)	320 nM(Ki)
JAK2 (Cell-free assay)	740 nM(Ki)