616431  Tranylcypromine, HCl

Histone Lysine Demethylase Inhibitor, LSD Inhibitor, Monoamine Oxidase Inhibitor II, Parnate, 2-PCPA, TCP, (1R)-2-Phenylcyclopropan-1-amine, HCl, trans-2-Phenylcyclopropylamine, HCl, BHC110 Inhibitor

A cell-permeable phenylcyclopropylamine that inhibits the monoamine oxidase and histone demethylase activities, respectively, of MAO A/B (K_i = 101.9 and 16.0 µM, respectively) and LSD1/2 (K_i = 242.7 and 180.0 µM, respectively), four members of a flavin-dependent amine oxidase family enzymes, by a covalent adduct formation with the enzyme-bound FAD. In addition to preventing LSD1-CoREST (Corepressor of RE1-Silencing Transcription factor) complex-mediated H3K4 demethylation (IC₅₀ < 2 µM), TCP also inhibits LSD1-HCF-1 (Host Cell Factor-1) complex-mediated H3K9 demethylase activity, which is demonstrated to be an essential mechanism for the replication and latent infection of the α-herpesviruses HSV and VZV. The combined treatment of 2 µM TCP and 10 µM CHIR99061 (Cat. No. 361559) is reported to enable the reprogramming of Oct4/Klf4-transduced primary HNEKs (Human Neonatal Epidermal Keratinocytes) into iPS (induced Pluripotent Stem) cells, albeit at a 100-time lower efficiency as seen in cultures transduced with 4-TFs (Oct44, Klf4, Sox2, and c-Myc).