货号 | 16178-5mg |
描述 | Janus-associated kinase 3 (JAK3) is a cytoplasmic protein tyrosine kinase that functions in the initiation of cytokine-triggered signal transduction by catalyzing the phosphorylation of signal transduction and activators of transcription. JAK3 is abundantly expressed in normal lymphoid cells as well as human lymphoblastic and myeloblastic leukemia cells. WHI-P154 is a quinazoline derivative that exhibits immunosuppressive effects by selectively inhibiting JAK3 (IC50 = 1.8 μM versusIC50s > 10 μM for JAK1 and JAK2).1 It has been reported to inhibit additional kinases including EGFR (IC50 = 4 nM) and VEGFR as well as the non-receptor tyrosine kinases, Abl, Lck, and Src.1 WHI-P154 is cytotoxic to human glioblastoma cells (IC50 = 813 nM) and has been used to induce the differentiation of neuronal precursor cells.2,3,4 |
别名 | JAK3 Inhibitor II;Janus-Associated Kinase 3 Inhibitor II; |
供应商 | Cayman |
应用文献 | |
1.Changelian, P.S.,Moshinsky, D.,Kuhn, C.F., et al. The specificity of JAK3 kinase inhibitors. Blood 111(4), 2155-2157 (2008). 2.Narla, R.K.,Liu, X.P.,Myers, D.E., et al. 4-(3-Bromo-4hydroxylphenyl)-amino-6,7-dimethoxyquinazoline: A novel quinazoline derivative with potent cytotoxic activity against human glioblastoma cells. Clinical Cancer Research 4(6), 1405-1414 (1998). 3.Narla, R.K.,Liu, X.P.,Klis, D., et al. Inhibition of human glioblastoma cell adhesion and invasion by 4-(4-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P131) and 4-(3-bromo-4-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P154). Clinical Cancer Research 4(10), 2463-2471 (1998). 4.Kim, Y.H.,Chung, J.I.,Woo, H.G., et al. Differential regulation of proliferation and differentiation in neural precursor cells by the Jak pathway. Stem Cells 28(10), 1816-1828 (2010). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 376.2 |
分子式 | C16H14BrN3O3 |
CAS号 | 211555-04-3 |
稳定性 | ≥ 2 years |
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