产品描述:
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).{18539} PP1 inhibits anti-CD3-induced tyrosine phosphorylation of human T cells with an IC50 value of 600 nM.{18539} 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.{22348,22349} 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.{22347}