1-Naphthyl PP1 selectively inhibits c-Src family kinases v-Src and Fyn (c-Fyn) as well as c-Abl tyrosine kinase (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, Fyn (c-Fyn), c-Abl, CDK2 and CAMK II respectively). 1-Naphthyl PP1 preferentially inhibits mutant over wild-type kinases (IC50 values are 1.5 vs 1000 nM for I338G v-src and v-src respectively).
1. Bishop et al (1999) Generation of monospecific nanomolar tyrosine kinase inhibitors via a chemical genetic approach. J.Am.Chem.Soc. 121 627. 2. Bishop, A.C. et al. 2000. Nature. 407(6802): 395-401. PMID: 11014197 3. Kenski, D.M. et al. 2005. J. Biol. Chem. 280(41): 35051-35061. PMID: 16081410 4. Endo, S. et al. 2006. Biochem. Biophys. Res. Commun. 341(1): 261-265. PMID: 16431218 5. Reboutier, D. et al. 2013. J. Cell Biol. 201(1): 65-79. PMID: 23547029
Soluble in DMSO (~20 mg/ml), chloroform, ethanol (~2 mg/ml), DMF (~30 mg/ml), and 1: 5 solution of DMF: PBS (pH 7.2) (~0.15 mg/ml).
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ReboutierReboutier, D. et al. (PubMed 23547029) reported the design of the first human Aurora A kinase (as-AurA) engineered by chemical genetics techniques. This kinase is fully functional biochemically and in cells, and is rapidly and specifically inhibited by the ATP analogue 1-Naphthyl-PP1 (1-Na-PP1). By treating cells exclusively expressing the as-AurA with 1-Na-PP1, they discovered that Aurora A is required for central spindle assembly in anaphase through phosphorylation of Ser 19 of P150Glued. -SCBT Publication Review
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