PP1 Analog II, 1NM-PP1 (CAS 221244-14-0)
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PP1 Analog II, 1NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors. It is an inhibitor of kinases that have been mutated, by a single base substitution, to become ′analog sensitive′, as compared to the wild-type kinase. PP1 Analog II, 1NM-PP1 was first developed to optimally inhibit v-Src-as1, with an I338G substitution, preferentially over v-Src (IC50 = 4.2 nM versus 28 muM, respectively). The homologous mutation in other kinases generated similar analog sensitivity (e.g., IC50 = 3.2 nM for c-Fyn-as1 versus 1.0 muM for c-Fyn 5.0 nM for CDK2-as1 versus 29 muM for CDK2 8.0 nM for CAMKII-as1 versus 24 muM for CAMKII). This approach has been used to elucidate functions of several kinases in both mammalian and yeast systems. In addition, it may act to activate mutants of Ire1, a transmembrane kinase.
PP1 Analog II, 1NM-PP1 (CAS 221244-14-0) References
- A chemical switch for inhibitor-sensitive alleles of any protein kinase. | Bishop, AC., et al. 2000. Nature. 407: 395-401. PMID: 11014197
- Chemical genetic analysis of the budding-yeast p21-activated kinase Cla4p. | Weiss, EL., et al. 2000. Nat Cell Biol. 2: 677-85. PMID: 11025657
- Bypassing a kinase activity with an ATP-competitive drug. | Papa, FR., et al. 2003. Science. 302: 1533-7. PMID: 14564015
- DNA end resection, homologous recombination and DNA damage checkpoint activation require CDK1. | Ira, G., et al. 2004. Nature. 431: 1011-7. PMID: 15496928
- Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells. | Larochelle, S., et al. 2007. Mol Cell. 25: 839-50. PMID: 17386261
- Alphaherpesvirus US3-mediated reorganization of the actin cytoskeleton is mediated by group A p21-activated kinases. | Van den Broeke, C., et al. 2009. Proc Natl Acad Sci U S A. 106: 8707-12. PMID: 19435845
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PP1 Analog II, 1NM-PP1, 1 mg | sc-203214 | 1 mg | $106.00 | |||
PP1 Analog II, 1NM-PP1, 5 mg | sc-203214A | 5 mg | $520.00 |