PP 1

PP 1 (CAS 172889-26-8) is a selective inhibitor targeting the Src family of non-receptor protein tyrosine kinases, including p56lck and p59fynT (IC50: 5 nM and 6 nM, respectively). Src kinases regulate signal transduction pathways influencing cell proliferation, migration, adhesion, and survival, making them important targets in cancer studies. In vitro, PP 1 selectively suppresses Lyn kinase in RBL-2H3 cells without affecting Syk kinase and effectively inhibits RET oncogene-driven transformation at nanomolar concentrations. In vivo, PP 1 reduces tyrosine phosphorylation events and T-cell proliferation, highlighting its utility in research on Src kinase function and signaling pathways in oncology and immunology.

References:

[1]Sen B and Johnson FM. Regulation of src family kinases in human cancers. J Signal Tr. 2010 Feb; doi:10.1155/2011/865819.

[2] Amoui M, Driber P and Driberovi L. Src family-selective tyrosine kinase inhibitor, PP1, inhibits both FcERI- and Thy-1-mediated activation of rat basophilic leukemia cells. Eur. J. Immunol. 1997. 27: 1881-1886.

[3]Carlomagno F, Vitagliano D, Guida T, Napolitano M, Vecchio G, Fusco A, Gazit A, Levitzki A and Santoro M. The kinase inhibitor PP1 blocks tumorigenesis induced by RET oncogenes. Cancer Res. 2002 Feb. 62: 1077–82