PP1, 1 mg

From STEMCELL Technologies, this small molecule 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, and is relatively selective for SRC family kinases versus other kinases, inhibiting EGFR, JAK2, and ZAP70 with IC₅₀ values of 0.25, > 50, and > 100 µM, respectively, and c-KIT, PDGFR, and RET tyrosine kinase in the 75 - 100 nM range. It also blocks TGF-β-mediated cellular responses by directly inhibiting type I TGF-β receptors (IC₅₀ = 50 nM).

Identified chemically as 4-Amino-5-(methylphenyl)-7-(t-butyl)pyrazolo-(3,4-d)pyrimidine (CAS 172889-26-8), the compound has the formula C₁₆H₁₉N₅, a molecular weight of 281.4 g/mol, and a purity of ≥ 98%. It is supplied as a white crystalline solid. Storage recommendations include keeping the product stable at -20°C as supplied, protected from prolonged exposure to light, with stability for 12 months from the date of receipt. Solubility is ≤ 3 mM in DMSO and ≤ 0.5 mM in absolute ethanol. The compound has low solubility in aqueous media.

Published applications include enabling reprogramming of mouse embryonic fibroblasts to induced pluripotent stem cells in the absence of the reprogramming factor SOX2, as well as 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.