Tranylcypromine Sulfate

Tranylcypromine Sulfate (CAS No.: 13492-01-8) is a synthetic small-molecule research reagent classified as an irreversible, nonselective monoamine oxidase inhibitor and a mechanism-based inhibitor of the flavin-dependent lysine-specific demethylase 1 (KDM1A/LSD1), widely used in neurochemical and epigenetic research as well as exploratory drug discovery screening; at the biochemical level, it simultaneously targets MAO-A and MAO-B, blocking the oxidative deamination of monoamine substrates, thereby modulating signaling pathways related to neurotransmitter turnover and affecting downstream gene regulatory networks; inhibition of LSD1 can reduce the demethylation of mono- and dimethylated lysine 4 on histone H3, perturb transcriptional programs associated with the CoREST complex, and thereby affect chromatin state and lineage differentiation processes. In terms of in vitro activity, depending on enzyme preparations from different sources, assay formats, and preincubation conditions, its apparent potency against MAO isoenzymes is typically in the submicromolar to micromolar range, while for LSD1 it is more often observed at low to mid micromolar levels, and it exhibits time-dependent inactivation characteristics consistent with the formation of a covalent adduct with the flavin cofactor. As a tool compound, it is commonly used to dissect monoamine metabolism in neuronal and peripheral cell systems, to study epigenetic control in development and differentiation models, and to establish and calibrate screening cascades for evaluating MAO or LSD1 target occupancy and functional linkage; in mechanistic studies using rodent animal models, it has also been used to examine phenotypes such as lesion growth and nociceptive sensitization, reflecting the systemic effects brought about by its dual activity. This compound is typically deployed in enzymatic assays, cell models, and animal studies to build structure-activity relationships, validate target dependence, and generate pharmacodynamic readouts (such as changes in histone methylation status or monoamine content); the concentrations or doses used in experiments should be determined according to the specific experimental design, biological system, and endpoint indicators. This product is for laboratory research only and is not intended for human or veterinary use.