Tranylcypromine . hemisulfate is a non-selective, irreversible monoamine oxidase inhibitor (MAOI), primarily used in research related to neuropsychiatric disorders. It is also a potent inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A), with an IC50 < 2 μM.
Key features and applications include:
- Dual Enzyme Inhibition: Irreversibly inhibits LSD1 (a histone demethylase) and MAO-A/B, impacting both epigenetic regulation and neurotransmitter metabolism.
- Epigenetic Modulation: Modulates gene expression by inhibiting LSD1, altering histone methylation patterns critical for chromatin remodeling and transcriptional regulation.
- Stem Cell Research: Maintains pluripotency, enhance chemical reprogramming efficiency, and direct differentiation – particularly into insulin-producing β-cells – making it valuable for regenerative medicine and disease modeling.
- Neurobiology & Behavior: As a non-selective MAOI, tranylcypromine hemisulfate is used to study monoaminergic signaling pathways involved in mood regulation, cognition, and neuropsychiatric disorders.
Research Applications:
- Epigenetic and transcriptional regulation studies
- Neural progenitor cell proliferation and differentiation
- Cancer biology, particularly in studies involving histone modification and gene expression regulation
- Stem cell reprogramming and differentiation protocols
Relevant disease states include:
- Major Depressive Disorder (MDD): Particularly effective in treatment-resistant or atypical depression, where other antidepressants have failed.
- Acute Myeloid Leukemia (AML): LSD1 is critical for maintaining the undifferentiated state of leukemic cells. Inhibition by tranylcypromine promotes differentiation and reduces proliferation.
- Small Cell Lung Cancer (SCLC): LSD1 inhibition has shown promise in preclinical models of SCLC, where it affects neuroendocrine differentiation and tumor growth.
- Prostate and Breast Cancer: LSD1 is implicated in hormone receptor signaling and epigenetic regulation in these cancers.
- Neurodegenerative Disorders: Due to its MAOI activity, tranylcypromine is also being explored in models of Parkinson’s disease and Alzheimer’s disease, where monoamine regulation is disrupted.
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Last modified: July 28, 2025