NU 6140

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Cat.No. 3301 - NU 6140 | C23H30N6O2 | CAS No. 444723-13-1
Description: Cdk2 inhibitor; also potent inhibitor of aurora kinase A and B
Chemical Name: 4-[[6-(Cyclohexylmethoxy)-1H-purin-2-yl]amino]-N,N-diethylbenzamide
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Reviews
Literature

Biological Activity

Cyclin-dependent kinase 2 (cdk2) inhibitor (IC50 values are 0.42 - 1.1 μM). Displays some selectivity for cdk2 (IC50 value = 0.94 μM for cdk4 and >2.3 μM for other cdks). Induces cell-cycle arrest at the G2-M phase. Potentiates the apoptotic effect of taxol (Cat. No. 1097) in HeLa cells; down-regulates the antiapoptotic protein survivin. Also potently inhibits aurora kinases (IC50 values are 0.035 and 0.067 μM for aurora kinase B and A, respectively).

Technical Data

M. Wt 422.52
Formula C23H30N6O2
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 444723-13-1
PubChem ID 10202471
InChI Key XHEQSRJCJTWWAH-UHFFFAOYSA-N
Smiles O=C(N(CC)CC)C(C=C4)=CC=C4NC1=NC(NC=N2)=C2C(OCC3CCCCC3)=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 42.25 100
ethanol 42.25 100

Preparing Stock Solutions

The following data is based on the product molecular weight 422.52. 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 2.37 mL 11.83 mL 23.67 mL
5 mM 0.47 mL 2.37 mL 4.73 mL
10 mM 0.24 mL 1.18 mL 2.37 mL
50 mM 0.05 mL 0.24 mL 0.47 mL

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References

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

Pennati et al (2005) Potentiation of PacT.-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol.Cancer.Ther. 4 1328 PMID: 16170024

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987


If you know of a relevant reference for NU 6140, please let us know.

View Related Products by Product Action

View all Cyclin-Dependent Protein Kinase Inhibitors

Keywords: NU 6140, NU 6140 supplier, NU6140, cdk2, inhibitor, cyclin-dependent, kinase, inhibitors, inhibits, anti-apoptotic, arrests, cell, cycle, Cyclin-dependent, Kinase, Aurora, Kinases, 3301, Tocris Bioscience

3 Citations for NU 6140

Citations are publications that use Tocris products. Selected citations for NU 6140 include:

Zhang et al (2016) miR-200b induces cell cycle arrest and represses cell growth in esophageal squamous cell carcinoma. Carcinogenesis 37 858 PMID: 27496804

Boekhout et al (2016) Feedback regulation between atypical E2Fs and APC/CCdh1 coordinates cell cycle progression. EMBO Rep 17 414 PMID: 26882548

Berenjeno et al (2017) Oncogenic PIK3CA induces centrosome amplification and tolerance to genome doubling. Nat Commun 8 1773 PMID: 29170395


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Literature in this Area

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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.