gapdh-in-1

GAPDH-IN-1 (Compound F8) is a GAPDH inhibitor, with an IC50 value of 39.31 μM for GAPDH enzyme activity. It forms a covalent adduct with the aspartic acid in the active site, displacing the enzyme's cofactor NAD+, and simultaneously enhances the reactivity of cysteine-reactive probes with the catalytic cysteine.

Malonyl-NAC increases cellular propylation, reducing endogenous GAPDH activity, increases GAPDH malonylation in cells, and inhibits pyruvate kinase activity. Additionally, malonyl-NAC limits the metabolism and proliferation of a highly glycolytic kidney cancer cell line harboring a tricarboxylic acid cycle mutation [1].