NU2058 NU2058 is a competitive inhibitor of CDK1/2 with respect to ATP. NU2058 is also shown to inhibit Topo II, affect p53-dependent transcription and halt cell growth at the G1 phase.

NU2058  (CAS 161058-83-9)

NU2058 is rated 5.0 out of 5 by 1.
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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 NAME CATALOG # UNIT PRICE QTY FAVORITES
NU2058 sc-202744 5 mg $87.00
NU2058 sc-202744A 25 mg $315.00

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.


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

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)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
UO7440420
PubChem CID :
4564
MDL Number :
MFCD05664734
SMILES :
C1CCC(CC1)COC2=NC(=NC3=C2NC=N3)N

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Certificate of Analysis

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Rated 5 out of 5 by from Harrison et al Harrison 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
Date published: 2015-05-04
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