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Literature summary for 4.2.99.18 extracted from

  • Bapat, A.; Glass, L.S.; Luo, M.; Fishel, M.L.; Long, E.C.; Georgiadis, M.M.; Kelley, M.R.
    Novel small molecule inhibitor of Ape1 endonuclease blocks proliferation and reduces viability of glioblastoma cells (2010), J. Pharmacol. Exp. Ther., 334, 988-998.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 4.2.99.18

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Rosetta cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2,4,9-trimethylbenzo[b][1,8]naphthyridin-5-amine i.e. Ape1 repair inhibitor 03, specific inhibitor of AP endonuclease Homo sapiens
2-(4-(2,5-dimethyl-1H-prryol-1-yl)phenoxy) acetic acid i.e. Ape1 repair inhibitor 01, specific inhibitor of AP endonuclease Homo sapiens
4-(2,6,8-trimethylquinolin-4-ylamino)phenol i.e. Ape1 repair inhibitor 02, specific inhibitor of AP endonuclease Homo sapiens
A1NI2-A3NI1
-
 Homo sapiens
N-(3-chlorophenyl)-5,6-dihyro-4H-cyclopenta[d]isoxazole-3-carboxamide i.e. Ape1 repair inhibitor 06, specific inhibitor of AP endonuclease Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA column chromatography, S-Sepharose column chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
glioblastoma cell
-
 Homo sapiens
-
SF-767 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DNA Ape1 cleaves the phosphodiester backbone 5' to the AP site generating 3'-hydroxyl and 5'-deoxyribosephosphate termini, Ape1 exhibits a prominent 5' hydrolytic AP endonuclease, a weak 3'-diesterase and a 3'-5'-exonuclease activity Homo sapiens fragments of DNA
-
 ?

Synonyms

Synonyms Comment Organism
AP endonuclease 1
-
 Homo sapiens
APE1
-
 Homo sapiens
apurinic/apyrimidinic endonuclease
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0016
-
-
 Homo sapiens N-(3-chlorophenyl)-5,6-dihydro-4H-cyclopenta[d]isoxazole-3-carboxamide
0.0017
-
-
 Homo sapiens [4-(2,5-dimethyl-1H-pyrrol-1-yl)phenoxy]acetic acid
0.0021
-
-
 Homo sapiens 2,4,9-trimethylpyridino[2,3-b]quinoline-5-ylamine
0.0064
-
-
 Homo sapiens 4-((2,6,8-trimethylquinolin-4-yl)amino)phenol