An irreversible

GSK-LSD1 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
2102933-95-7
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

An irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM); induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s <5 nM)

Formal name: rel-N-[(1R,2S)-2-phenylcyclopropyl]-4-piperidinamine, dihydrochloride

Synonyms: 

Molecular weight: 289.2

CAS: 2102933-95-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Demethylation

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