WHI-P 154 is a JAK3 inhibitor (IC50 = 1.8 μM) that displays no activity at JAK1 or JAK2. WHI-P 154 inhibits STAT1 activation, iNOS expression, and NO production in macrophages in vitro. WHI-P 154 induces apoptosis in human glioblastoma cell lines (IC50 = 158 μM). WHI-P 154 inhibits other common kinases including EGFR (IC50 = 4 nM), SRC, c-Abl, VEGFR, MAPK and PI 3-kinase.
Narla et al (1998) 4-(3'-bromo-4'hydroxylphenyl)-amino-6,7-dimethoxyquinazoline: a novel quinazoline derivative with potent cytotoxic activity against human glioblastoma cells. Clin.Cancer Res. 4 1405. Sareila et al (2008) Janus kinase 3 inhibitor WHI-P154 in macrophages activated by bacterial endotoxin: differential effects on the expression of iNOS, COX-2 and TNF-α. Int.Immunopharmacol. 8 100. Changelian et al (2008) The specificity of JAK3 kinase inhibitors. Blood 111 2155.
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