KU-0060648

SKU: orb1300661

Description

KU-0060648 is a potent small molecule inhibitor that primarily targets DNA-PK and the PI3Kα, β, and δ isoforms with low nanomolar IC₅₀ values, while showing significantly weaker activity against PI3Kγ. This profile makes it a useful research tool for investigating DNA damage response and PI3K signaling pathways in both cellular and animal models of cancer and other diseases.

Research Area

Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 881375-00-4
• MW: 582.71
• Purity: 98.75%
• Formula: C₃₃H₃₄N₄O₄S
• SMILES: CCN1CCN(CC(=O)Nc2ccc(-c3cccc4c3oc(cc4=O)N3CCOCC3)c3sc4ccccc4c23)CC1
• Target: PI3K,mTOR,DNA-PK

Bioactivity

• Target IC50:
  PI3Kγ:0.594 μM|DNA-PK:8.6 nM|PI3Kα:4 nM|PI3Kβ:0.5 nM|PI3Kδ:0.1 nM
• In Vivo:
  KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model.
• In Vitro:
  KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only by 55% in SW620 cells. In clonogenic survival assays, KU-0060648 increases the cytotoxicity of etoposide and doxorubicin across the panel of DNA-PKcs-proficient cells, but not in DNA-PKcs-deficient cells, confirming that enhanced cytotoxicity of the topoisomerase II poisons etoposide and doxorubicin is due to DNA-PK inhibition.
• Cell Research:
  SRB assay(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KU0060648, KU-0060648, KU 0060648, inhibit, mTOR, Inhibitor, Mammalian target of Rapamycin, DNA-dependent protein kinase, DNAPK, DNA-PK, PI3K, PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, Phosphoinositide 3-kinase

Compound Identifiers

PubChem CID

11964036