NU 2058

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Cat.No. 3135 - NU 2058 | C12H17N5O | CAS No. 161058-83-9
Description: Cdk1 and cdk2 inhibitor
Chemical Name: 6-(Cyclohexylmethoxy)-9H-purin-2-amine
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (4)

Biological Activity

Cyclin-dependent kinase (cdk) 1 and cdk2 inhibitor (Ki values are 5 and 12 μM respectively). Inhibits growth of human tumor cells in vitro (mean GI50 = 13 μM). Also inhibits DNA topoisomerase II ATPase activity (IC50 = 300 μM).

Compound Libraries

NU 2058 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 247.3
Formula C12H17N5O
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 161058-83-9
PubChem ID 4564
InChI Key MWGXGTJJAOZBNW-UHFFFAOYSA-N
Smiles NC1=NC(OCC3CCCCC3)=C2C(NC=N2)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 24.73 100
ethanol 2.47 10

Preparing Stock Solutions

The following data is based on the product molecular weight 247.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.04 mL 20.22 mL 40.44 mL
5 mM 0.81 mL 4.04 mL 8.09 mL
10 mM 0.4 mL 2.02 mL 4.04 mL
50 mM 0.08 mL 0.4 mL 0.81 mL

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References

References are publications that support the biological activity of the product.

Arris et al (2000) Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J.Med.Chem. 43 2797 PMID: 10956187

Knockaert et al (2002) Pharmacological inhibitors of cyclin-dependent kinases. TiPS 23 417 PMID: 12237154

Jensen et al (2005) Substituted purine analogues define a novel structural class of catalytic topoisomerase II inhibitors. Cancer Res. 65 7470 PMID: 16103101


If you know of a relevant reference for NU 2058, please let us know.

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View all Cyclin-Dependent Protein Kinase Inhibitors

Keywords: NU 2058, NU 2058 supplier, Cdk1, cdk2, Topoisomerase, II, inhibits, inhibitors, Cyclin-Dependent, Protein, Kinases, DNA, Isomerases, NU2058, Cyclin-dependent, Kinase, 3135, Tocris Bioscience

1 Citation for NU 2058

Citations are publications that use Tocris products. Selected citations for NU 2058 include:

Goonesekere et al (2014) A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers. PLoS One 9 e93046 PMID: 24740004


Do you know of a great paper that uses NU 2058 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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Cancer

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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.