NU-2058

SKU: orb1226060

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).

Key Properties

• CAS Number: 161058-83-9
• MW: 247.2963
• Purity: >98% (HPLC)
• Formula: C₁₂H₁₇N₅O
• SMILES: NC1=NC(OCC2CCCCC2)=C3N=CNC3=N1
• Target: CDK
• Solubility: DMSO: ≥ 32 mg/mL

Bioactivity

• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

O6-cyclohexylmethyl guanine | NU2058 | NU 2058

Quick Database Links

Gene Symbol

CDK