tcsc1662 PP1

PP1 is a potent, and Src family-selective tyrosine kinase inhibitor with IC₅₀ of 5 and 6 nM for Lck and Fyn, respectively.

IC50 & Target: IC50: 5 nM (Lck), 6 nM (Fyn), 250 nM (EGFR), >50 μM (JAK2)^[1]

In Vitro: 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^[1].