CRT0044876

SKU: orb1300753

Description

CRT0044876

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 6960-45-8
• MW: 206.15
• Purity: 98.27% (May vary between batches)
• Formula: C₉H₆N₂O₄
• SMILES: OC(=O)c1cc2cccc([N+]([O-])=O)c2[nH]1
• Target: DNA/RNA Synthesis
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (9.7 mM);DMSO:40 mg/mL (194.03 mM);Ethanol:1 mg/mL (4.85 mM)

Bioactivity

• Target IC50:
  APE1:3 μM
• In Vitro:
  CRT0044876 potently inhibits the AP endonuclease, 3'-phosphodiesterase and 3'-phosphatase activities of APE1, and exhibits the selectivity for the inhibition of exonuclease III family. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds with an accumulation of unrepaired AP sites. CRT0044876, by inhibition of the BER pathway increases oxidative DNA damage temporally related to increased intracellular reactive oxygen species in an acidic tumor microenvironment, and thus results in cell cycle arrests and increased DNA double strand breaks, leading to cell death.
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• Cell Research:
  HT1080 fibrosarcoma cells are grown in 2% RPMI medium [supplemented with penicillin 0.06 g/l, streptomycin 0.1 g/l (pH 7.0), 10% fetal bovine serum and 4 mM glutamine]. Only cells with a plating efficiency of ≥60% are used for clonogenic survival analysis. Tissue culture dishes (10 cm) are seeded with 500 cells per dish and the culture is maintained in a humidified incubator at 37°C in an atmosphere of 5% CO2 and 95% air. To evaluate the toxicity profile of putative APE1 inhibitors, various concentrations (100–500 μM) of inhibitor are added to the medium, and cultures were incubated for 7-10 days until cell colonies are formed. Colonies are fixed [75% (v/v) methanol, 25% (v/v) acetic acid] for 30 min and stained with crystal violet (1 mg/ml in distilled water) for 4 h at room temperature. Visible colonies are counted on a colony counter. (Only for Reference)
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Storage & Handling

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

Alternative Names

DNA/RNA Synthesis, DNA Synthesis, DNASynthesis, CRT0044876, CRT-0044876, CRT 0044876, APE1, base, 7-Nitroindole-2-Carboxylic Acid, 7-NO2-ICA, NSC69877, NSC-69877, NSC 69877, NSC 69877,7-NO2-ICA, non-toxic, endonuclease, exonuclease, excision, RNASynthesis, RNA Synthesis

Compound Identifiers

PubChem CID

81409