PP1

PP1 is a reversible inhibitor of the SRC family of tyrosine kinases. It inhibits LCK, FYN, HCK and SRC with IC₅₀ values of 5, 6, 20 and 170 nM, respectively (Hanke et al.). It is relatively selective for SRC family kinases versus other kinases, inhibiting epidermal growth factor receptor (EGFR), janus-activated kinase 2 (JAK2) and zeta-chain-associated protein kinase 70 (ZAP70) with IC₅₀ values of 0.25, > 50, and > 100 μM, respectively, and KIT, platelet-derived growth factor receptor (PDGFR), and RET tyrosine kinase in the 75 - 100 nM range (Carlomagno et al. ; Tatton et al.; Waltenberger et al.; Hanke et al.). PP1 also blocks TGF-β-mediated cellular responses by directly inhibiting type I TGF-β receptors (IC₅₀ = 50 nM; Ungefroren et al.; Maeda et al.).

REPROGRAMMING

• Enables reprogramming of mouse embryonic fibroblasts to induced pluripotent stem cells in the absence of reprogramming factor SOX2 (Staerk et al.; Ma et al.).

CANCER RESEARCH

• Blocks TGF-β-mediated migration of primary non-small cell lung carcinoma cells and pancreatic ductal adenocarcinoma cell lines (Bartscht et al.).
• Induces apoptosis in non-small cell lung cancer cell lines (Zhang et al.).