Preferred Label : APE1/Ref-1 Redox Inhibitor APX3330;
NCIt synonyms : APE1/Ref-1 Inhibitor APX3330; [(2E)-2-[(4,5-dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]-undecanoic
Acid;
NCIt related terms : APX-3330;
NCIt definition : An orally bioavailable inhibitor of apurinic/apyrimidinic endonuclease 1/reduction-oxidation
(redox) effector factor-1 (APE1/Ref-1; APEX1), with potential anti-angiogenic and
antineoplastic activities. Upon administration, the APE1/Ref-1 Inhibitor APX3330 selectively
targets and binds to APE1/Ref-1. This inhibits the redox-dependent signaling activity
of APE1/Ref-1, by preventing the reduction and activation of numerous APE1/Ref-1-dependent
oncogenic transcription factors (TFs), such as nuclear factor kappa B (NF-kB), AP-1,
STAT3, p53, NRF2 and HIF-1alpha, that are involved in signaling, cell proliferation,
tumor progression and survival of cancer cells. Therefore, this agent inhibits the
activation of multiple TF-mediated signaling pathways and inhibits tumor cell proliferation
and survival. APE1/Ref-1, a multifunctional protein overexpressed in many cancer cell
types, plays a key role as a redox regulator of transcription factor activation and
in base excision repair upon DNA damage. It drives cancer cell proliferation, migration,
drug resistance, angiogenesis and inflammation and its expression level correlates
with increased tumor aggressiveness and decreased patient survival. APX3330 specifically
blocks the redox activity of APE1/Ref-1 and does not affect its ability to act as
a DNA repair endonuclease.;
UNII : 11267UI968;
CAS number : 136164-66-4; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 136164-66-4
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G-SRS /a ;
Molecule name : E3330; E 3330; APX 3330; APX-3330;
NCI Metathesaurus CUI : CL551955;
Origin ID : C150216;
UMLS CUI : C4725663;
Semantic type(s)
- concept_is_in_subset
- has_target
