262015

DNA Base Excision Repair Pathway Inhibitor

The DNA Base Excision Repair Pathway Inhibitor, also referenced under CAS 6960-45-8, controls the biological activity of APE1 (human apurinic/apyrimidinic endonuclease.

• Synonym(s): DNA Base Excision Repair Pathway Inhibitor, 7-Nitroindole-2-carboxylic acid, CRT0044876
• Empirical Formula (Hill Notation): C₉H₆N₂O₄
• CAS Number: 6960-45-8
• Molecular Weight: 206.15
• MDL number: MFCD00044720
• UNSPSC Code: 12352200
• NACRES: NA.54

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: tan
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [N+](=O)([O-])c1c2[nH]c(cc2ccc1)C(=O)[O-]
• InChI: 1S/C9H6N2O4/c12-9(13)6-4-5-2-1-3-7(11(14)15)8(5)10-6/h1-4,10H,(H,12,13)/p-1
• InChI key: BIUCOFQROHIAEO-UHFFFAOYSA-M

Description

General description

A cell-permeable, potent, specific, and nontoxic inhibitor of the DNA repair enzyme, APE1 (human apurinic/apyrimidinic endonuclease; IC₅₀ = ~3 µM). Shown to target the APE1 active site and inhibit its 3′-phosphodiesterase and 3′-phosphatase activities. Exhibits minimal effects on endonuclease IV, BamH1 restriction endonuclease, or topoisomerase I even at concentration as high as 100 µM. Also shown to potentiate the cytotoxicity of several DNA damaging agents, such as MMS, temozolomide, Zeocin, and H₂O₂ in HeLa, HT1080, and MDA-MB-231 cells.

A cell-permeable, potent, specific, and nontoxic inhibitor of the DNA repair enzyme, APE1 (human apurinic/apyrimidinic endonuclease; IC₅₀ ~3 µM). Shown to target the APE1 active site and inhibit its 3′-phosphodiesterase and 3′-phosphatase activities. Exhibits minimal effects on endonuclease IV, BamH1 restriction endonuclease, or topoisomerase I even at concentration as high as 100 µM. Also shown to potentiate the cytotoxicity of several DNA damaging agents, such as MMS, temozolomide, Zeocin, and H₂O₂ in HeLa, HT1080, and MDA-MB-231 cells.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
APE 1

Product does not compete with ATP.

Reversible: no

Target IC₅₀: ~3 µM against APE1 (human apurinic/apyrimidinic endonuclease

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Madhusudan, S., et al. 2005. Nucl. Acids Res.33, 4711.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Pictograms: GHS08
• Signal Word: Danger
• Hazard Statements: H319,H334
• Precautionary Statements: P261 - P264 - P280 - P284 - P305 + P351 + P338 - P337 + P313
• Hazard Classifications: Eye Irrit. 2 - Resp. Sens. 1
• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable