JAK - JAK3

GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively.

BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.

JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM).

NVP-BSK805 dihydrochloride (BSK805 dihydrochloride) is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.