General description
A cell-permeable phenylcyclopropylamine that inhibits the monoamine oxidase and histone demethylase activities, respectively, of MAO A/B (Ki = 101.9 and 16.0 M, respectively) and LSD1/2 (Ki = 242.7 and 180.0 M, 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 M), 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 M TCP and 10 M CHIR99061 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).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Liang, Y., et al. 2009. Nat. Med.15, 1312.Li, W., et al. 2009. Stem Cells27, 2992.Karytinos, A., et al. 2009. J. Biol. Chem.284, 17775.Hruschka, S., et al. 2008. Bioorg. Med. Chem.16, 7148.Schmidt, D.M., and McCafferty, D.G. 2007. Biochemistry46, 4408.Lee, M.G., et al. 2006. Chem. Biol.13, 563.Yoshida, S., et al. 2004. Bioorg. Med. Chem.12, 2645.
Packaging
Packaged under inert gas
500 mg in Glass bottle
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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