PENAO

PENAO is a novel, proprietary small molecule anti-cancer compound and a second-generation peptide arsenical derived from GSAO. It contains an active arsenic moiety that disrupts mitochondrial function in cancer cells by inhibiting the adenine nucleotide translocase (ANT), a key protein involved in mitochondrial ADP/ATP exchange. This disruption leads to mitochondrial dysfunction, proliferation arrest, and cell death in tumor cells. PENAO accumulates in cells much faster than its predecessor GSAO and demonstrates significantly increased anti-proliferative activity and anti-tumor efficacy in preclinical models. It has shown synergistic effects when combined with mTOR inhibitors or EGFR inhibitors, enhancing tumor cell death through multiple mechanisms including apoptosis and autophagy[1][3][5][6][8].

Other names

4-(N-(S-penicillaminylacetyl)amino)phenylarsonous acid3-((2-((4-(dihydroxyarsino)phenyl)amino)-2-oxoethyl)thio)-D-valine(2S)-2-amino-3-((((4-(dihydroxyarsanyl)phenyl)carbamoyl)methyl)sulfanyl)-3-methylbutanoic acid