CRT0044876

SKU: orb1221869

Description

CRT0044876 is a potent BER inhibitor or DNA Base Excision Repair Pathway Inhibitor (APE1 IC50 - 3 microM). CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds, with accumulation of apurinic sites.

Key Properties

• CAS Number: 6960-45-8
• MW: 206.15
• Purity: >98% (HPLC)
• Formula: C₉H₆N₂O₄
• SMILES: OC(=O)C1=CC2=C(N1)C(=CC=C2)[N+]([O-])=O
• Target: APE1
• Solubility: In Vitro: DMSO : 50 mg/mL (242.54 mM)

Bioactivity

• In Vitro:
  A key step in BER is the processing of an apurinic/apyrimidinic (AP) site intermediate by an AP endonuclease. CRT0044876 has an IC50 for inhibition of APE1 of ~3 μM and not only inhibits AP site cleavage catalyzed by purified APE1, but also cleavage directed by APE1 in a HeLa whole cell extract. CRT0044876 inhibits the 3′-phosphoglycolate diesterase activity of APE1 with an IC50 of ~5 μM. CRT0044876 inhibits both the exonuclease and AP endonuclease activities of exonuclease III, but shows no inhibitory activity towards endonuclease IV. CRT0044876 has minimal effects on BamHI restriction endonuclease or topoisomerase I even at CRT0044876 concentrations of 100 μM. At non-toxic concentrations, CRT0044876 potentiates the cytotoxicity of several DNA damaging agents, which generate damage that is repaired in the BER pathway, including some currently-used anticancer drugs. The combination of MMS and CRT0044876 leads to a synergistic increase in the level of AP sites. Consistent with CRT0044876 being a specific BER inhibitor, a strong potentiation of hmdUrd cytotoxicity is seen in CRT0044876-treated cells (HT1080 cells).
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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

CRT0044876 | CRT-0044876 | CRT 0044876

Quick Database Links

Gene Symbol

APE1