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CRT0044876

Catalog No. T6456 CAS 6960-45-8

Synonyms: NSC 69877,7-NO2-ICA, NSC 69877, 7-Nitroindole-2-Carboxylic Acid

CRT0044876 (7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

CRT0044876, CAS 6960-45-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 30.00
10 mg	In stock	$ 38.00
25 mg	In stock	$ 61.00
50 mg	In stock	$ 85.00
100 mg	In stock	$ 108.00
200 mg	In stock	$ 135.00
500 mg	In stock	$ 223.00
1 mL * 10 mM (in DMSO)	In stock	$ 39.00

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Purity: 98%

Purity: 97.79%

Biological Description

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Description	CRT0044876 (7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM.
Targets&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. [1] 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. [2]
Kinase Assay	AP site cleavage assay: BER reaction buffer comprises 40 mM HEPES–KOH (pH 7.8), 5 mM MgCl2, 0.5 mM DTT and 0.1 mM EDTA. A 10 μl AP site cleavage reaction comprised of BER buffer mix, purified protein (3.3 nM final concentration of APE1) and 0.75 ng reduced AP site double-stranded oligonucleotide. The mixture is incubated at 37°C for 1 h. A total of 1 μl of stop buffer (50% glycerol, 10 mM Tris–HCl, 1 mM EDTA, 0.1% bromophenol blue and 0.1% Xylene cyanol) is added, and the sample mixture is denatured at 90–100°C for 2 min. The sample is then run on a 15% TBE Criterion? Pre-Cast Gel, with electrophoresis at a constant current of 30 mA for 30 min, and the radiolabeled substrate and reaction products are visualized using a phosphorImager. The inhibitory activity of potential APE1-targeting compounds are analyzed at drug concentrations ranging from 0.1 to 100 μM. The resolved radiolabeled bands are quantified using ImageQuant software analysis, and IC50 values are calculated by determining the concentration of the inhibitor that reduced APE1 activity to 50% of the control values.
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)

Synonyms	NSC 69877,7-NO2-ICA, NSC 69877, 7-Nitroindole-2-Carboxylic Acid
Molecular Weight	206.15
Formula	C9H6N2O4
CAS No.	6960-45-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 39 mg/mL (189.2 mM)

Ethanol: 1 mg/mL (4.85 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Madhusudan S, et al. Nucleic Acids Res. 2005, 33(15), 4711-4724. 2. Seo Y, et al. Cancer Res. 2009, 69(18, 7285-7293. 3. Long K, Gu L, Li L, et al. Small-molecule inhibition of APE1 induces apoptosis, pyroptosis, and necroptosis in non-small cell lung cancer[J]. Cell Death & Disease. 2021, 12(6): 1-15.

Citations

1. Long K, Gu L, Li L, et al. Small-molecule inhibition of APE1 induces apoptosis, pyroptosis, and necroptosis in non-small cell lung cancer. Cell Death & Disease. 2021, 12(6): 1-15. 2. Du Y, Zhou Y, Yan X, et al.APE1 inhibition enhances ferroptotic cell death and contributes to hepatocellular carcinoma therapy.Cell Death & Differentiation.2024: 1-16.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Anti-Aging Compound Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Cancer Compound Library Target-Focused Phenotypic Screening Library Cell Cycle Compound Library DNA Damage & Repair Compound Library NO PAINS Compound Library

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Keywords

CRT0044876 6960-45-8 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis CRT-0044876 non-toxic CRT 0044876 DNA NSC 69877,7-NO2-ICA Inhibitor base exonuclease inhibit NSC 69877 7-Nitroindole-2-Carboxylic Acid endonuclease NSC-69877 excision NSC69877 repair inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.