CS12192 is a potent, selective JAK3/JAK1/TBK1 inhibitor with IC50 of 11/105/162 nM, respectively.
CS12192 inhibits Flt4 with IC50 of 107 nM, weakly inhibits JAK2 with an IC50 of 1404 nM.
CS12192 shows slightly over 50% of inhibitory activity only to a few other kinases (such as BMX, FLT3, KDR, but not TYK2) in an activity screening assay for a panel of 75 human kinases.
CS12192 inhibits IL-2 stimulation induced a clear phosphorylation of STAT1, 3, and 5 in KHYG-1 cell line.
CS12192 is a selective inhibitor against JAK3/JAK1, but not JAK2.
CS12192 suppresses IFN gene expression through the inhibition of TBK1 signaling pathway.
CS12192 (80 mg/kg) ameliorates disease severity of both AIA and CIA in rats.
