Search Ontology:
ChEBI

Pac-1

Term ID
CHEBI:231696
Synonyms
  • PAC 1
  • PAC1
  • Procaspase activating compound 1
  • Procaspase-3 Activator
Definition
Procaspase Activating Compound-1 VO-100 is an orally bioavailable procaspase activating compound-1 (PAC-1), with potential proapoptotic and antineoplastic activities. Upon administration, VO-100 binds to and forms a chelating complex with zinc (Zn) ions inside cells, which prevents the binding of Zn ions to procaspase-3 (PC3) and abrogates the Zn-mediated inhibition of PC3. This allows for the proteolytic autoactivation of PC3 into the active form caspase-3. This results in the selective caspase-3-mediated induction of apoptosis and cell death in cancer cells. In addition, VO-100 is able to cross the blood-brain-barrier (BBB). PC3, a Zn-inhibited proenzyme, is upregulated in a variety of cancer cell types, while its expression is minimal in normal healthy cells.
References
  • cas:315183-21-2
Ontology
ChEBI  ( EBI )
Relationships
Phenotype
Phenotype resulting from Pac-1
Phenotype where environments contain Pac-1
Phenotype modified by environments containing Pac-1
Phenotype affecting Pac-1
Human Disease Model