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NU2058 (CAS 161058-83-9)

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Application:A CDK1, CDK2, and Topo II inhibitor
CAS Number:161058-83-9
Molecular Weight:247.3
Molecular Formula:C12H17N5O
Refer to Certificate of Analysis for lot specific data (including water content).
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 Ordering Information
Product NameCatalog #UnitPriceQtyAddFavorites
NU2058 sc-202744 5 mg $87
NU2058 sc-202744A 25 mg $315
Description
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.
Technical Information
Physical State:Solid
Solubility:Soluble in DMSO (100 mM), water, and ethanol (10 mM).
Storage:Store at 4° C
Melting Point:205.85 °C (Predicted) (tautomer)
Boiling Point:580.76 °C at 760 mmHg (Predicted) (tautomer)
Density:1.3 g/cm3 (Predicted) (tautomer)
Refractive Index:n20D 1.65 (Predicted)
IC50:Cdk1/cyclin B: IC50 = 5 µM; Cdk1: IC50 = 7 µM (human); Cdk2/cyclin A: IC50 = 12 µM; Cdk2: IC50 = 17 µM (human); MCF7: IC50 = 24.2 µM (human)
Ki Data:Cdk2: Ki= 1.2 µM (human); Cdk1: Ki= 5 µM; Cdk1/cyclin B1: Ki= 5 µM (human); Cdk2/cyclin A: Ki= 12 µM (human)
pK Values:pKa: 9.21 (Predicted), pKb: 3.22 (Predicted)
Safety and Reference Information
WGK Germany:3
RTECS:UO7440420
PubChem CID:4564
MDL Number:MFCD05664734
SMILES:C1CCC(CC1)COC2=NC(=NC3=C2NC=N3)N
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
References
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
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