PP1 is a selective and potent Src-family tyrosine kinase inhibitor. PP1 studies have proved its ability to potently inhibit Lck and Fyn (FynT), IL-2 gene activation in T lymphocytes, and anti-CD3-induced protein tyrosine phosphorylation. Research indicates that PP1 effectively blocks LPA and EGF-enhanced tyrosine phosphorylation, MAPK activation downstream of EGFR, Rsk-1 (p90RSK) activation by H2O2, Kit and Bcr-Abl tyrosine kinases, and degrades RETMEN2A and RETMEN2B oncoproteins via proteosomal targeting. PP1 and its analog, PP2, are powerful inhibitors of TGF-β-induced cell migration and invasion in-vitro. PP1 inhibits anti-CD3-induced T cell tyrosine phosphorylation, TcR-induced T cell proliferation, and IL-2 gene induction. PP1 has been demonstrated to reduce the expression of vascular endothelial growth factor (VEGF), protect the blood-brain barrier, reduce brain edema immediately after subarachnoid hemorrhage, and offer cerebral protection against stroke. It prevents metastatic spread in late-stage pancreatic ductal adenocarcinoma and non-small cell lung cancer.
Peptides & proteins
AGL-1872, PP 1, 1-tert-butyl-3-(4-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine
1) Hanke, JH., et al. 1996. J Biol Chem. 271(2): 695-701. PMID: 8557675; 2) Carlomagno, F., et al. 2002. Cancer Res. 62(4): 1077-1082. PMID: 11861385; 3) Zhang, Y., et al. 2012. Genes Dev. 26(1): 69-81. PMID: 22215812; 4) Ma, T., et al. 2013. Circ Res. 112(3): 562-574. PMID: 23371904
-20°C. Keep away from direct sunlight.
12 months from receipt