NU6102 (CAS 444722-95-6)
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NU6102 stands out as an potent inhibitor of cyclin-dependent kinases 1 and 2 (CDK1/cyclin B and CDK2/cyclin A3), with inhibitory concentrations (IC50 values) demonstrating a thousand-fold greater potency (IC50 ≤ 9.5 nM for CDK1/cyclin B and IC50 = 5.4 nM for CDK2/cyclin A3) when compared to NU2058. This marked potency underscores the molecule′s targeted efficacy against these specific kinases, which are pivotal in the regulation of cell cycle progression and DNA repair processes. The selectivity of NU6102 is further highlighted by its significantly lesser inhibitory effect on other kinases such as CDK4/D1 (IC50 = 1.6 µM), DYRK1A (IC50 = 0.9 µM), PDK1 (IC50 = 0.8 µM), and ROCKII (IC50 = 0.6 µM), indicating a focused action on CDK1 and CDK2.
NU6102 (CAS 444722-95-6) References
- 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
- 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
- High affinity targets of protein kinase inhibitors have similar residues at the positions energetically important for binding. | Sheinerman, FB., et al. 2005. J Mol Biol. 352: 1134-56. PMID: 16139843
- Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. | Pratt, DJ., et al. 2006. J Med Chem. 49: 5470-7. PMID: 16942020
- 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
- Preclinical in vitro and in vivo evaluation of the potent and specific cyclin-dependent kinase 2 inhibitor NU6102 and a water soluble prodrug NU6301. | Thomas, HD., et al. 2011. Eur J Cancer. 47: 2052-9. PMID: 21570822
- Identification and Characterization of an Irreversible Inhibitor of CDK2. | Anscombe, E., et al. 2015. Chem Biol. 22: 1159-64. PMID: 26320860
- Differential Regulation of Progesterone Receptor-Mediated Transcription by CDK2 and DNA-PK. | Treviño, LS., et al. 2016. Mol Endocrinol. 30: 158-72. PMID: 26652902
- Combined PI3K and CDK2 inhibition induces cell death and enhances in vivo antitumour activity in colorectal cancer. | Beale, G., et al. 2016. Br J Cancer. 115: 682-90. PMID: 27529512
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
NU6102, 1 mg | sc-222082 | 1 mg | $55.00 | |||
NU6102, 5 mg | sc-222082A | 5 mg | $122.00 |