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Submit ReviewWHI-P 154 is a 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.
分子量 | 376.2 |
公式 | C16H14BrN3O3 |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 211555-04-3 |
PubChem ID | 3795 |
InChI Key | CBIAKDAYHRWZCU-UHFFFAOYSA-N |
Smiles | OC(C=C3)=C(Br)C=C3NC2=NC=NC1=CC(OC)=C(OC)C=C12 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: WHI-P 154, WHI-P 154 supplier, JAK3, kinases, inhibitors, inhibits, EGFR, Potent, Janus, Activated, Kinases, Epidermal, Growth, Factor, Receptors, ErbB, Her, Receptor, Tyrosine, RTKs, WHIP154, JAK, Kinase, Neural, Stem, Cells, 3115, Tocris Bioscience
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