| Identification | Back Directory | [Name]
LSD1-IN-1 | [CAS]
1431326-61-2 | [Synonyms]
RG 6016
CS-1530
ORY-1001
LSD1-IN-1
ORY-1001 (RG-6016)
ORY-1001 2HCl salt
ORY-1001(LSD1-IN-1)
ORY-1001 (RG-6016) 2HCl
LSD1-IN-1;ORY1001;ORY 1001
ORY-1001 trans and cis isomers
RG 6016;RG6016;RG-6016;ORY1001;ORY 1001
rel-N1-[(1R,2S)-2-Phenylcyclopropyl]-1,4-cyclohexanediamine hydrochloride
rel-N1-[(1R,2S)-2-Phenylcyclopropyl]-1,4-cyclohexanediamine hydrochloride (1:2) | [Molecular Formula]
C15H24Cl2N2 | [MDL Number]
MFCD28900684 | [MOL File]
1431326-61-2.mol | [Molecular Weight]
303.27 |
| Hazard Information | Back Directory | [Description]
Lysine-specific demethylase 1 (LSD1) demethylates H3K4 and H3K9, resulting in transcriptional repression.1 It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).2 ORY-1001 is an orally available, selective inhibitor of LSD1 (IC50 < 20 nM).3,4 It targets acute myeloid leukemia (AML) stem cells and significantly reduces tumor cell load while increasing survival time in mouse models of AML.3,4 ORY-1001 is in clinical trials for cancer treatment.4 | [Uses]
ORY-1001 is a potent LSD1 inhibitor. | [in vitro]
ory-1001 is an enantiomerically pure kdm1a inhibitor with high selectivity against related fad dependent aminoxidases. ory-1001 does not inhibit non-related histone modifiers, and is clean in a cerep diversity panel. treatment of thp-1 cells with ory-1001, results in a time/dose dependent me2h3k4 accumulation at kdm1a target genes and concomitant induction of differentiation markers [1]. | [in vivo]
daily oral administration of doses < 0.020 mg/kg leads to significantly reduced tumor growth in rodent xenografts. in vivo studies have shown that ory-1001 presents excellent oral bioavailability, target exposure and activity in vivo [1]. | [IC 50]
<20nm | [storage]
Store at -20°C | [References]
[1] tamara maes, i?igo tirapu, cristina mascaró, alberto ortega, angels estiarte, nuria valls, julio castro-palomino, carlos buesa arjol, guido kurz; oryzon genomics, s. a., cornella de llobregat. preclinical characterization of a potent and selective inhibitor of the histone demethylase kdm1a for mll leukemia. j clin oncol 31, 2013 (suppl; abstr e13543). |
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