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Literature summary for 4.2.99.18 extracted from

  • Simeonov, A.; Kulkarni, A.; Dorjsuren, D.; Jadhav, A.; Shen, M.; McNeill, D.R.; Austin, C.P.; Wilson, D.M.
    Identification and characterization of inhibitors of human apurinic/apyrimidinic endonuclease APE1 (2009), PLoS ONE, 4, e5740.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 4.2.99.18

Inhibitors

Inhibitors Comment Organism Structure
6-hydroxy-DL-DOPA complete inhibition at 0.1 mM Homo sapiens
aurintricarboxylic acid potent inhibitor of APE1 Homo sapiens
ceftriaxone sodium
-
 Homo sapiens
cephapirin sodium
-
 Homo sapiens
Mitoxantrone
-
 Homo sapiens
additional information hiolactomycin and methyl 3,4-dephostatin have no effect on total AP site cleavage activity Homo sapiens
myricetin above 80% inhibition at 0.1 mM Homo sapiens
NSC-13755 complete inhibition at 0.1 mM Homo sapiens
Reactive blue 2 above 80% inhibition at 0.1 mM Homo sapiens
tyrphostin AG 538 mild inhibition at 0.1 mM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.065
-
 1-amino-4-(4-{(E)-[(4E)-6-chloro-4-[(3-sulfophenyl)imino]-3,4-dihydro-1,3,5-triazin-2(1H)-ylidene]amino}-3-sulfoanilino)-9,10-dioxo-9,10-dihydroanthracene-2-sulfonic acid
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293T cell
-
 Homo sapiens
-
HeLa cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DNA
-
 Homo sapiens fragments of DNA
-
 ?
Reactive Blue 2
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
APE1
-
 Homo sapiens
human apurinic/apyrimidinic endonuclease
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0005
-
 IC50 less than 0.0005 mM Homo sapiens myricetin
0.0005
-
 IC50 less than 0.0005 mM Homo sapiens Reactive blue 2
0.0005
-
 IC50 less than 0.0005 mM Homo sapiens mitoxanthrone
0.0005
-
 IC50 less than 0.0005 mM Homo sapiens 6-hydroxy-DL-DOPA
0.05
-
 IC50 above 0.05 mM Homo sapiens cephapirin sodium
0.05
-
 IC50 above 0.05 mM Homo sapiens ceftriaxone sodium

General Information

General Information Comment Organism
physiological function APE1 is the major nuclease for excising abasic sites and particular 3'-obstructive termini from DNA, and is an integral participant in the base excision repair pathway Homo sapiens