Chemical Name:1-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazolo[3,
4-d]pyrimidin-4-amine
Biological Activity:
Potent inhibitor of Src-family tyrosine kinases.
Inhibits p56lck and p59fynT(IC50
values are 5 and 6 nM respectively). Displays > 8000-fold selectivity over
ZAP-70 and Jak2. Also moderately inhibitσp38, CSK, PDGF
receptors,
RET-derived oncoproteins, c-Kit and Bcr-Abl.
Hankeet al
(1996) Discovery of a novel, potent, and src family-selective tyrosine kinase
inhibitor. J.Biol.Chem. 271 695. Liuet al (1999)
Structural basis for selective inhibition of Src family kinases by PP1.
Chem.Biol. 6 671. Carlomagnoet al (2002) The
kinase inhibitor PP1 blocks tumorigenesis induced by RET oncogenes.
Cancer Res. 62 1077.Bain et al
(2003) The
specificities of protein kinase inhibitors: an update. Biochem.J. 371
199. Tatton et al (2003) The src-selective kinase inhibitor PP1 also
inhibits Kit and Bcr-Abl tyrosine kinases. J.Biol.Chem. 278 4847.
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