JAK3 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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 376.2. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.66 mL||13.29 mL||26.58 mL|
|5 mM||0.53 mL||2.66 mL||5.32 mL|
|10 mM||0.27 mL||1.33 mL||2.66 mL|
|50 mM||0.05 mL||0.27 mL||0.53 mL|
References are publications that support the biological activity of the product.
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
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
Changelian et al (2008) The specificity of JAK3 kinase inhibitors. Blood 111 2155 PMID: 18094329
Kim et al (2010) Differential regulation of proliferation and differentiation in neural precursor cells by the Jak pathway. Stem Cells. 28 1816 PMID: 20979137
If you know of a relevant reference for WHI-P 154, please let us know.
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