Cayman PP1 (Src Inhibitor)

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

WARNING This product is not for human or veterinary use.