NU-2058 is an ATP-competitive inhibitor of CDK1 and CDK2 with Ki of 5 uM and 12 uM respectively.
NU-2058 inhibits human tumor cells with a mean GI50 of 13±7 uM.
NU-2058 reduces CDK2-mediated phosphorylation of pRb, E2F transcriptional activity and proliferatio in both anti-estrogen-sensitive and resistant cells.
NU-2058 also inhibits DNA topoisomerase II ATPase activity (IC50=300 uM).
Physicochemical Properties
M.Wt
247.2963
Formula
C12H17N5O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
DMSO: ≥ 32 mg/mL
Chemical Name/SMILES
9H-Purin-2-amine, 6-(cyclohexylmethoxy)-
References
1. Arris CE, et al. J Med Chem. 2000 Jul 27;43(15):2797-804.
2. Johnson N, et al. Br J Cancer. 2010 Jan 19;102(2):342-50.
3. Harrison LR, et al. Biochem Pharmacol. 2009 May 15;77(10):1586-92.
