| 货号 | 13330-25mg |
| 描述 | 1-NM-PP1 is a cell permeable inhibitor of kinases that have been mutated, by a single base substitution, to become ‘analog sensitive’ (as), as compared to the wild-type kinase. 1-NM-PP1 was first developed to optimally inhibit v-Src-as1, with an I338G substitution, preferentially over v-Src (IC50 = 4.2 nM versus 28 μM, respectively).1 The homologous mutation in other kinases generated similar analog sensitivity (e.g.,IC50 = 3.2 nM for c-Fyn-as1 versus 1.0 μM for c-Fyn; 5.0 nM for Cdk2-as1 versus 29 μM for Cdk2; 8.0 nM for CAMKII-as1 versus 24 μM for CAMKII).2 This approach has been used to elucidate functions of several kinases in both mammalian and yeast systems.2,3,4,5,6 |
| 别名 | PP1 Analog II; |
| 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.Weiss, E.L.,Bishop, A.C.,Shokat, K.M., et al. Chemical genetic analysis of the budding-yeast p21-activated kinase Cla4p. Nature Cell Biology 2, 677-685 (2000). 4.Ira, G.,Pellicioli, A.,Balijja, A., et al. DNA end resection, homologous recombination and DNA damage checkpoint activation require CDK1. Nature 431, 1011-1017 (2004). 5.Larochelle, S.,Merrick, K.A.,Terret, M.E., et al. Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells. Molecular Cell 25(6), 839-850 (2007). 6.Van den Broeke, C.,Radu, M.,Deruelle, M., et al. Alphaherpesvirus US3-mediated reorganization of the actin cytoskeleton is mediated by group A p21-activated kinases. Proceedings of the National Academy of Sciences of the United States of America 106(21), 8707-8712 (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 331.4 |
| 分子式 | C20H21N5 |
| CAS号 | 221244-14-0 |
| 稳定性 | ≥ 2 years |
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