| 货号 | 10954-1mg |
| 描述 | 1-NA-PP1 is a reversible, cell-permeable inhibitor of Src-family tyrosine kinases that have been mutated, by a single base substitution, to become ‘analog sensitive’ (as), as compared to the wild-type kinase. 1-NA-PP1 was first developed to optimally inhibit v-Src-as1, with an I338G substitution, preferentially over v-Src (IC50 = 1.5 nM versus 1.0 μM, respectively).1 The homologous mutation in other kinases generated similar analog sensitivity (e.g.,IC50 = 1.5 nM for c-Fyn-as1 versus 0.6 μM for c-Fyn; 7.0 nM for c-Abl-as2 versus 0.6 μM for c-Abl; 15 nM for Cdk2-as1 versus 18 μM for Cdk2).2 This approach has been used to elucidate functions of several kinases in both mammalian and yeast systems.2,3,4 |
| 别名 | 1-Naphthyl-PP1;PP1 Analog; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Bishop, A.C.,Kung, C.y.,Shah, K., et al. Generation of monospecific nanomolar tyrosine kinase inhibitors via a chemical genetic approach. Journal of the American Chemical Society 121, 627-631 (1999). 2.Bishop, A.C.,Ubersax, J.A.,Petsch, D.T., et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature 407, 395-401 (2000). 3.Endo, S.,Satoh, Y.,Shah, K., et al. A single amino-acid change in ERK1/2 makes the enzyme susceptible to PP1 derivatives. Biochemical and Biophysical Research Communications 341, 261-265 (2006). 4.Kenski, D.M.,Zhang, C.,von Zastrow, M., et al. Chemical genetic engineering of G protein-coupled receptor kinase 2. The Journal of Biological Chemisty 280(41), 35051-35061 (2005). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 317.4 |
| 分子式 | C19H19N5 |
| CAS号 | 221243-82-9 |
| 稳定性 | ≥ 2 years |
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