GSK-LSD1 A chemical probe for LSD1

Click Cayman Chemical,  Sigma or Tocris to obtain this probe


GSK-LSD1 (trans-racemic)
MW 216.3
FW  289.2 (di-HCl)

Lysine specific demethylase 1 (LSD1) is a histone demethylase found in various transcriptional co-repressor complexes. LSD1 is involved in ES cell differentiation, hematopoiesis, and has been described as having a role in Acute Myeloid Leukemia (AML). GlaxoSmithKline has developed an irreversible, mechanism based inhibitor of LSD1, GSK-LSD1, and has made this available as a chemical probe as part of the SGC epigenetics initiative. GSK-LSD1 inhibits LSD1 with an IC50 of 16 nM and is > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B).  GSK-LSD1 induces gene expression changes in cancer cell lines (average EC50 < 5 nM) and inhibits cancer cell line growth (average EC50 < 5 nM). 

LSD-1 at 10 µM showed no activity against 55 human recombinant receptors in the CEREP ExpresSProfile selectivity/specificity profile (GPCR, transporters, ion channels), except 5-HT1A (49% inhibition) 5-HT transporter (74% inhibition) and dopamine transporter (39 % inhibition). 



Physical and chemical properties for GSK-LSD1
Molecular weight216.2
Molecular formulaC14H20N2
IUPAC nameN-(2-phenyl-cyclopropyl)-piperidin-4-amine
No. of chiral centres2
No. of rotatable bonds3
No. of hydrogen bond acceptors2
No. of hydrogen bond donors2
  • C1CNCCC1N[C@@H]1C[C@H]1c1ccccc1
  • InChI:
  • InChI=1S/C14H20N2/c1-2-4-11(5-3-1)13-10-14(13)16-12-6-8-15-9-7-12/h1-5,12-16H,6-10H2/t13-,14+/m0/s1
  • InChI Key:
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