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-3 (Compound 1), an APE1 inhibitor, is utilized in cancer research.

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].

S-Adenosyl-L-methionine disulfate tosylate (Ademetionine disulfate tosylate) is the disulfate-tosylate mixed salt comprising diastereoisomers of ademetionine ions. Ademetionine exhibits anti-inflammatory properties and has been utilized in the treatment of chronic liver disease.

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

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

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).

7-Hydroxyaristolochic acid A is a natural derivative of aristolochic acid. Aristolochic acid is nephrotoxic and carcinogenic, inhibits APE1 Nrf2 HO-1 axis-induced oxidative stress and apoptosis leading to nephrotoxicity, and induces apoptosis in NRK-52E cells via COX-2 and PGE2.

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

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

Lucanthone (Lucanthonum) is an inhibitor of Apurinic endonuclease-1 (APE-1).

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.