| 货号 | 14244-1mg |
| 描述 | The Src family of non-receptor tyrosine kinases regulate cell adhesion, growth, and differentiation through activation of multiple intracellular signaling pathways. Normally inactive, Src kinases are transiently activated during mitosis and constitutively activated by abnormal mutations. PP1 is a potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. It inhibits p56lck (IC50 = 5 nM), p59fynT (IC50 = 6 nM), Hck (IC50 = 20 nM), and Src (IC50 = 170 nM) without significantly affecting the activity of EGFR kinase (IC50 = 250 nM), JAK2 (IC50 = 50 µM), or ZAP-70 (IC50 ≥ 0.6 µM).1 PP1 inhibits anti-CD3-induced tyrosine phosphorylation of human T cells with an IC50 value of 600 nM.1 It exhibits antitumor activity by antagonizing both proliferation and the inhibition of apoptosis mediated by a stem cell factor/mast cell growth factor in hematopoietic and small cell lung cancer cell lines.2,3 PP1 also blocks TGF-β-mediated cellular responses by directly inhibiting type I TGF-β receptors (IC50 = 50 nM) in a manner unrelated to Src signaling.4 |
| 别名 | AGL 1872;EI 275; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Hanke, J.H.,Gardner, J.P.,Dow, R.L., et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. The Journal of Biological Chemisty 271(2), 695-701 (1996). 2.Krystal, G.W.,DeBerry, C.S.,Linnekin, D., et al. Lck associates with and is activated by kit in a small cell lung cancer cell line: Inhibition of SCF-mediated growth by the Src family kinase inhibitor PP1. Cancer Research 58, 4660-4666 (1998). 3.Tatton, L.,Morley, G.M.,Chopra, R., et al. The Src-selective kinase inhibitor PP1 also inhibits kit and Bcr-Abl tyrosine kinases. The Journal of Biological Chemisty 278(7), 4847-4853 (2003). 4.Ungefroren, H.,Sebens, S.,Groth, S., et al. The Src family kinase inhibitors PP2 and PP1 block TGFβ-mediated cellular responses by direct and differential inhibition of type I and type II TGFβreceptors. Current Cancer Drug Targets 11(4), 524-535 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 281.4 |
| 分子式 | C16H19N5 |
| CAS号 | 172889-26-8 |
| 稳定性 | ≥ 2 years |
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