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
- UPC:
- 51241817
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 262015-25MG
- CAS:
- 6960-45-8
