3-(4-Chlorophenyl)-1-(1,1-dimethylethyl)-1H-pyrazolo(3,4-d)pyrimidin-4-amine

개요The 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. PP2 is a potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. It inhibits p56lck (IC50 = 4 nM), p59fynT (IC50 = 5 nM), Hck (IC50 = 5 nM), and Src (IC50 = 100 nM). PP2 does not significantly affect the activity of EGFR kinase (IC50 = 480 nM), JAK2 (IC50 > 50 μM), or ZAP-70 (IC50 > 100 μM). PP2 inhibits the activation of focal adhesion kinase as well as its phosphorylation at Tyr577. PP2 also inhibits anti-CD3-stimulated tyrosine phosphorylation of human T-cells with an IC50 value of 600 nM.

용도PP2 has been used:to analyze the effects of Src/focal adhesion kinase (FAK) signaling on IQ domain GTPase-activating protein 1 (IQGAP1)-mediated anoikis resistancefor Src inhibition to study its effect on epidermal growth factor receptor (EGFR) and nuclear factor erythroid 2-related factor 2 (Nrf2) phosphorylation in non-small cell lung cancer (NSCLC) cellsfor pharmacological inhibition of SRC in MDA-MB-231 breast cancer cells