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
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 37 In Stock
10MG 33 In Stock
25MG 67 In Stock
50MG 100 In Stock
100MG 152 In Stock
200MG 226 In Stock
500MG 369 In Stock
1G Get Quote In Stock

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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