Src is the best understood member of a family of 9 tyrosine kinases that regulates cellular responses to extracellular stimuli. The Src family of non-receptor tyrosine kinases are integrators of divergent signal transduction pathways which regulate numerous cellular processes, including tumorigenicity and angiogenesis[3]. Dysfunction of Src, through overexpression or increased activation, has profound effects on basic cellular functions. Elevated Src expression and/or activation is evident across a wide range of solid tumour types.[4]. PP1 is a potent, and Src family-selective tyrosine kinase inhibitor with IC50 of 5 and 6 nM for Lck and Fyn, respectively. PP1 inhibits Lck (IC50=5 nM) and FynT (IC50=6 nM) in vitro at concentrations significantly lower than those required to inhibit ZAP-70 (IC50>100 μM), JAK2 (IC50>50 μM), the EGFR kinase, and protein kinase A. PP1 inhibits whole cell tyrosine phosphorylation and proliferation in T cells stimulated with anti-CD3 and mitogens. PP1 selectively inhibits IL-2 gene expression over GM-CSF and IL-2R gene induction in human T cells[5]. 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[6].
PP1 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
Jurkat cells
Function assay
Inhibition of MLR stimulated IL-2 production in Jurkat cells, IC50=0.4 μM
11012021
mouse NIH/3T3 cells
0.08-20 μM
Function assay
Inhibition of v-Src phosphorylation expressed in mouse NIH/3T3 cells at 0.08 to 20 uM by Western blot analysis
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