Cat. No. 3115
Chemical Name: 2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol
Biological ActivityJAK3 inhibitor (IC50 = 1.8 μM) that displays no activity at JAK1 or JAK2. Inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro. Also inhibits other common kinases including EGFR (IC50 = 4 nM), Src, Abl, VEGFR, MAPK and PI 3-K and induces apoptosis in human glioblastoma cell lines (IC50 = 158 μM). Induces differentiation of neural progenitor cells.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
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. PMID: 9626456.
Changelian et al (2008) The specificity of JAK3 kinase inhibitors. Blood 111 2155. PMID: 18094329.
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. PMID: 18068105.
Kim et al (2010) Differential regulation of proliferation and differentiation in neural precursor cells by the Jak pathway. Stem Cells. 28 1816. PMID: 20979137.
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Keywords: WHI-P 154, supplier, JAK3, kinases, inhibitors, EGFR, Potent, Janus, Activated, Kinases, Epidermal, Growth, Factor, Receptors, ErbB, Her, Receptor, Tyrosine, RTKs, WHIP154
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