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Submit ReviewNU 6140 is a 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).
NU 6140 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 42.25 | 100 | |
ethanol | 42.25 | 100 |
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 |
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.
Keywords: NU 6140, NU 6140 supplier, NU6140, cdk2, inhibitor, cyclin-dependent, kinase, inhibitors, inhibits, anti-apoptotic, arrests, cell, cycle, Cyclin-dependent, Kinase, Aurora, Kinases, CDK1, Subfamily, 3301, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for NU 6140 include:
Berenjeno et al (2017) Oncogenic PIK3CA induces centrosome amplification and tolerance to genome doubling. Nat Commun 8 1773 PMID: 29170395
Musa et al (2019) Cooperation of cancer drivers with regulatory germline variants shapes clinical outcomes. Nat Commun 10 4128 PMID: 31511524
Boekhout et al (2016) Feedback regulation between atypical E2Fs and APC/CCdh1 coordinates cell cycle progression. EMBO Rep 17 414 PMID: 26882548
Zhang et al (2016) miR-200b induces cell cycle arrest and represses cell growth in esophageal squamous cell carcinoma. Carcinogenesis 37 858 PMID: 27496804
Do you know of a great paper that uses NU 6140 from Tocris? Please let us know.
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