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NU-2058

CAS No. 161058-83-9

NU-2058( O6-cyclohexylmethyl guanine | NU2058 | NU 2058 )

Catalog No. M12326 CAS No. 161058-83-9

An ATP-competitive inhibitor of CDK1 and CDK2 with Ki of 5 uM and 12 uM respectively; inhibits human tumor cells with a mean GI50 of 13±7 uM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    NU-2058
  • Note
    Research use only, not for human use.
  • Brief Description
    An ATP-competitive inhibitor of CDK1 and CDK2 with Ki of 5 uM and 12 uM respectively; inhibits human tumor cells with a mean GI50 of 13±7 uM.
  • Description
    An ATP-competitive inhibitor of CDK1 and CDK2 with Ki of 5 uM and 12 uM respectively; inhibits human tumor cells with a mean GI50 of 13±7 uM; reduces CDK2-mediated phosphorylation of pRb, E2F transcriptional activity and proliferatio in both anti-estrogen-sensitive and resistant cells; also inhibits DNA topoisomerase II ATPase activity (IC50=300 uM).
  • In Vitro
    NU2058 (O6-(Cyclohexylmethyl)guanine) is a competitive inhibitor of CDK2 with respect to ATP (Ki value CDK2, 12 μM) that binds in the ATP binding pocket in a different orientation from other purine-based inhibitors, including olomoucine and roscovotine. NU2058 is the lead compound in a structure-based drug discovery program to develop more potent and selective CDK inhibitors.
  • In Vivo
    ——
  • Synonyms
    O6-cyclohexylmethyl guanine | NU2058 | NU 2058
  • Pathway
    Angiogenesis
  • Target
    CDK
  • Recptor
    CDK1|CDK2|TopoII
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    161058-83-9
  • Formula Weight
    247.2963
  • Molecular Formula
    C12H17N5O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 32 mg/mL
  • SMILES
    NC1=NC(OCC2CCCCC2)=C3N=CNC3=N1
  • Chemical Name
    9H-Purin-2-amine, 6-(cyclohexylmethoxy)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Arris CE, et al. J Med Chem. 2000 Jul 27;43(15):2797-804. 2. Johnson N, et al. Br J Cancer. 2010 Jan 19;102(2):342-50. 3. Harrison LR, et al. Biochem Pharmacol. 2009 May 15;77(10):1586-92.
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