PP1, 10 mg

STEMCELL Technologies offers PP1, a reversible small-molecule 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. The compound is relatively selective for SRC family 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 c-KIT, platelet-derived growth factor receptor (PDGFR), and RET tyrosine kinase in the 75–100 nM range. PP1 also blocks TGF-β-mediated cellular responses by directly inhibiting type I TGF-β receptors (IC₅₀ = 50 nM).

PP1 is supplied as a white crystalline solid with a purity of ≥ 98%. Its chemical name is 4-Amino-5-(methylphenyl)-7-(t-butyl)pyrazolo-(3,4-d)pyrimidine, with the molecular formula C₁₆H₁₉N₅ and a molecular weight of 281.4 g/mol (CAS number 172889-26-8). The compound is soluble in DMSO at ≤ 3 mM and in absolute ethanol at ≤ 0.5 mM, and has low solubility in aqueous media. The product is stable at -20°C as supplied (protected from prolonged exposure to light) for 12 months from date of receipt. As a general guide, resuspending 1 mg in 3.55 mL of DMSO yields a 1 mM stock solution. Stock solutions should be prepared fresh, stored in DMSO at -20°C, aliquoted to avoid repeated freeze-thaw cycles, and diluted into culture medium immediately before use; the final DMSO concentration should not exceed 0.1% due to potential cell toxicity.

Published applications include enabling reprogramming of mouse embryonic fibroblasts to induced pluripotent stem cells in the absence of the reprogramming factor SOX2, blocking TGF-β-mediated migration of primary non-small cell lung carcinoma cells and pancreatic ductal adenocarcinoma cell lines, and inducing apoptosis in non-small cell lung cancer cell lines. The product is classified as hazardous; users are referred to the Safety Data Sheet (SDS) and is intended for research use only.