JAK3-IN-2 is a potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM.
JAK3-IN-2 dispalys >4,300-fold selectivity over JAK1, JAK2 and TYK2, and other kinases BMX, EGFR, ITK and BTK.
JAK3-IN-2 blocks cytokine signaling through JAK3, but not through other JAK family enzymes.
JAK3-IN-2 inhibits IL-7 induced pSTAT5 in CD3+, CD8+ T cells with IC50 of 280 nM.
JAK3-IN-2 sufficiently blocks the development of inflammation in a rat model of rheumatoid arthritis, while sparing hematopoiesis.
