Cat. No. 3115
Chemical Name: 2-Bromo-4-[(6,7-dimethoxy-4-quinazo
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.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Kim et al (2010) Differential regulation of proliferation and differentiation in neural precursor cells by the Jak pathway. Stem Cells. 28 1816. PMID: 20979137.
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.
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.
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Keywords: WHI-P 154, supplier, JAK3, kinases, inhibitors, inhibits, EGFR, Potent, Janus, Activated, Kinases, Epidermal, Growth, Factor, Receptors, ErbB, Her, Receptor, Tyrosine, RTKs, WHIP154, Tocris Bioscience, EGFR Inhibitor products
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July 8 - 12, 2017