Molecular structure of NU2058, CAS Number: 161058-83-9
NU2058 (CAS 161058-83-9)
See product citations (2)
Alternate Names:
O6-Cyclohexylmethylguanine
Application:
NU2058 is a CDK1, CDK2, and Topo II inhibitor
CAS Number:
161058-83-9
Purity:
≥95%
Molecular Weight:
247.3
Molecular Formula:
C12H17N5O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
NU2058, also known as 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.
NU2058 (CAS 161058-83-9) References
- Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. | Arris, CE., et al. 2000. J Med Chem. 43: 2797-804. PMID: 10956187
- Structure-based design of cyclin-dependent kinase inhibitors. | Davies, TG., et al. 2002. Pharmacol Ther. 93: 125-33. PMID: 12191605
- Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor. | Davies, TG., et al. 2002. Nat Struct Biol. 9: 745-9. PMID: 12244298
- Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2. | Sayle, KL., et al. 2003. Bioorg Med Chem Lett. 13: 3079-82. PMID: 12941338
- The development of a CDK2-docking site peptide that inhibits p53 and sensitizes cells to death. | Ferguson, M., et al. 2004. Cell Cycle. 3: 80-9. PMID: 14657672
- N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2. | Hardcastle, IR., et al. 2004. J Med Chem. 47: 3710-22. PMID: 15239650
- Substituted purine analogues define a novel structural class of catalytic topoisomerase II inhibitors. | Jensen, LH., et al. 2005. Cancer Res. 65: 7470-7. PMID: 16103101
- Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer. | Rigas, AC., et al. 2007. Oncogene. 26: 7611-9. PMID: 17599054
- The kinase inhibitor O6-cyclohexylmethylguanine (NU2058) potentiates the cytotoxicity of cisplatin by mechanisms that are independent of its effect upon CDK2. | Harrison, LR., et al. 2009. Biochem Pharmacol. 77: 1586-92. PMID: 19426695
- Pre-clinical evaluation of cyclin-dependent kinase 2 and 1 inhibition in anti-estrogen-sensitive and resistant breast cancer cells. | Johnson, N., et al. 2010. Br J Cancer. 102: 342-50. PMID: 20010939
- Effect of cell cycle arrest on intermediate metabolism in the marine diatom Phaeodactylum tricornutum. | Kim, J., et al. 2017. Proc Natl Acad Sci U S A. 114: E8007-E8016. PMID: 28874574
- Blockade of Nuclear β-Catenin Signaling via Direct Targeting of RanBP3 with NU2058 Induces Cell Senescence to Suppress Colorectal Tumorigenesis. | Zheng, CC., et al. 2022. Adv Sci (Weinh). 9: e2202528. PMID: 36270974
- A computational ONIOM model for the description of the H-bond interactions between NU2058 analogues and CDK2 active site | Jans H. Alzate-Morales a, Julio Caballero a, Fernando D. Gonzalez-Nilo a, Renato Contreras b. 2009. Chemical Physics Letters. 479: 149-155.
Inhibitor of:
ACAT-3, Cdc28, Cdk1, Cdk10, Cdk2, Clb2, cyclin A, cyclin B, MGMT, Rad9B, ROGDI, and SHPRH.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
NU2058, 5 mg | sc-202744 | 5 mg | $66.00 | |||
NU2058, 25 mg | sc-202744A | 25 mg | $321.00 |