GSK-<wbr/>LSD1 (hydro<wbr>chloride)

GSK-LSD1 (hydrochloride)

CAT N°: 16439
Price:

From 48.00 40.80

Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).{12422} LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.{27091} GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s Structural Genomics Consortium (SGC) website for more information.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • rel-N-[(1R,2S)-2-phenylcyclopropyl]-4-piperidinamine, dihydrochloride
  • Correlated keywords
    • 1431368-48-7 1431367-49-5 1247999-77-4 1431367-50-8 1431367-51-9 epigenetic lysine specific demethylase 1 LSD1 transcriptional repression tumor p53 demethylation inhibit inhibitor one flavin adenine dinucleotide dinucleotide-dependent dependent FAD-dependent amine oxidase monoamine MAOs polyamine PAOs monomethylated dimethylated histone H3 4 four suppressor activity p53 residues LYS370 mechanism-based gene expression cancer cell line proliferation Structural Genomic Consortium SGC
  • Product Overview:
    Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).{12422} LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.{27091} GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s Structural Genomics Consortium (SGC) website for more information.

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