ape1

APE1-IN-1 is a potent inhibitor of purine pyrimidine endonuclease 1 (APE1) that crosses the blood-brain barrier, exhibits potential antitumor activity, and enhances the cytotoxicity of the alkylating agent [methyl methanesulfonate] on cancer cells.

APE1-IN-2 (compound AP1), a Pt(IV) proagent, selectively targets the essential base excision repair protein apurinic apyrimidinic endonuclease 1 (APE1). Exhibiting anticancer properties, APE1-IN-2 prompts the intracellular accumulation of platinum and initiates the activation of DNA damage response and apoptosis pathways [1].

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

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

Hycanthone (Etrenol(mesylate)) is a potent drug of antischistosomal. Hycanthone is a DNA intercalator that inhibits RNA synthesis and DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits APE1 via direct protein binding(KD: 10 nM).

APX2009 is a second-generation APE1/Ref-1 redox-specific inhibitor. APX2009 significantly reduces NFkB transcriptional activity, survivin mRNA, and survivin protein levels. APX2009 decreases prostate cancer cell proliferation and induces cell cycle arrest.

It is an inhibitor of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)

6-Hydroxy-DOPA is an allosteric inhibitor of RAD52, it inhibits proliferation of BRCA-deficient cancer cells in vitro and also inhibits APE1.