A potent Cdk1 and Cdk2 inhibitor
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NU 6102

Item No. 13317

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[6-(cyclohexylmethoxy)-9H-purin-2-yl]amino]-benzenesulfonamide
CAS Number
444722-95-6
Molecular Formula
C18H22N6O3S
Formula Weight
402.5
Purity
≥90%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: >1 mg/mlEthanol: >1 mg/ml
λmax
309 nm
SMILES
NS(C(C=C1)=CC=C1NC2=NC(NC=N3)=C3C(OCC4CCCCC4)=N2)(=O)=O
InChi Code
InChI=1S/C18H22N6O3S/c19-28(25,26)14-8-6-13(7-9-14)22-18-23-16-15(20-11-21-16)17(24-18)27-10-12-4-2-1-3-5-12/h6-9,11-12H,1-5,10H2,(H2,19,25,26)(H2,20,21,22,23,24)
InChi Key
OWXORKPNCHJYOF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $60

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    5 mg

    $185

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    Product Description

    NU 6102 is a potent inhibitor of Cdk1 and Cdk2 with Ki values of 9 and 6 nM and IC50 values of 9.5 and 5.4 nM, respectively.1,2 NU 6102 inhibits Cdk4 activity with an IC50 value of 1.6 μM, suggesting it is most selective for Cdk2.3 Time-lapse videomicroscopy reveals that 20 μM NU 6102 delays cell entry into mitosis where most cells appear to eventually complete mitotic division but cannot correctly undergo cytokinesis, and hence become binucleated with an abnormal number of centrosomes.4 In SKUT-1B cancer cells a 24 h exposure to NU 6102 induced G2 arrest, inhibition of target protein phosphorylation, and cytotoxicity with an LC50 value of 2.6 μM.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sayle, K.L., Bentley, J., Boyle, F.T., et al. Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2. Bioorg. Med. Chem. Lett. 13(18), 3079-3082 (2003).

    2. Hardcastle, I.R., Arris, C.E., Bentley, J., et al. N2-substituted O6-cyclohexylmethylguanine derivatives: Potent inhibitors of cyclin-dependent kinases 1 and 2. J. Med. Chem. 47(15), 3710-3722 (2004).

    3. Pratt, D.J., Bentley, J., Jewsbury, P., et al. Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. J. Med. Chem. 49(18), 5470-5477 (2006).

    4. Krasinska, L., Cot, E., and Fisher, D. Selective chemical inhibition as a tool to study Cdk1 and Cdk2 functions in the cell cycle. Cell Cycle 7(12), 1702-1708 (2008).

    5. Thomas, H.D., Wang, L.Z., Roche, C., et al. Preclinical in vitro and in vivo evaluation of the potent and specific cyclin-dependent kinase 2 inhibitor NU6102 and a water soluble prodrug NU6301. Eur. J. Cancer 47(13), 2052-2059 (2011).