NU2058, O(6)-Cyclohexylmethylguanine, has displayed the capacity to competitively inhibit CDK1 and CDK2 with respect to ATP and has also been shown to inhibit Topo II ATPase activity. Studies suggest that NU2058 also modifies p53-dependent transcription and interrupts the cell cycle causing cell growth arrest. NU2058 demonstrates the ability to alter the transport of platinum-based compounds via an increase in DNA adducts, which causes an increase in intracellular platinum levels. Further experiments reveal that growth inhibition caused by NU2058 is correlated to an increase in p27 levels, a decrease in early gene expression and CDK2 activity, as well as G1 cell cycle arrest. NU2058 is an inhibitor of cyclin A and cyclin B.
1. Arris, C.E., et al. 2000. J. Med. Chem. 43: 2797-2804. PMID: 10956187
2. Ferguson, M., et al. 2004. Cell Cycle. 3: 80-89. PMID: 14657672
3. Rigas, A.C., et al. 2007. Oncogene. 26: 7611-7619. PMID: 17599054
4. Harrison, L.R., et al. 2009. Biochem. Pharmacol. 77: 1586-1592. PMID: 19426695
Soluble in DMSO (100 mM), water, and ethanol (10 mM).
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Rated 5 out of
Harrison et alHarrison et al. (PubMed ID 19426695) found that NU2058 enhanced cisplatin toxicity by altering cisplatin transport and causing more Pt-DNA adducts, as well as sensitizing cells to cisplatin- and melphalan-induced DNA damage. -SCBT Publication Review
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