WHI-P97

Description: WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal. Target: JAK. Smiles: COc1cc2ncnc(Nc3cc(Br)c(O)c(Br)c3)c2cc1OC. References: Sudbeck EA, Liu XP, Narla RK, Mahajan S, Ghosh S, Mao C, Uckun FM.Structure-based design of specific inhibitors of Janus kinase 3 as apoptosisinducing antileukemic agents.Clin Cancer Res. 1999 Jun,5(6):1569-82.