1431303-72-8

1431303-72-8 structure

Name: ORY-1001(trans)
Chemical Name: ORY-1001(trans)
CAS Number: 1431303-72-8
Molecular Formula: C₁₅H₂₄Cl₂N₂
Molecular Weight: 303.271
Catalog: Signaling Pathways Epigenetics Histone Demethylase
Create Date: 2018-04-14 00:53:54
Modify Date: 2024-01-07 10:28:59
ORY-1001 trans is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.

Name	ORY-1001(trans)
Synonyms	trans-N-[(1R,2S)-2-Phenylcyclopropyl]-1,4-cyclohexanediamine dihydrochloride 1,4-Cyclohexanediamine, N1-[(1R,2S)-2-phenylcyclopropyl]-, trans-, hydrochloride (1:2)

Description	ORY-1001 trans is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
Related Catalog	Signaling Pathways >> Epigenetics >> Histone Demethylase Research Areas >> Cancer
Target	KDM1A/LSD1[1]
In Vitro	ORY-1001 trans is a KDM1A inhibitor that inactivate KDM1A by irreversible binding to the flavin adenine nucleotide (FAD) cofactor. ORY-1001 trans has very high selectivity for KDM1A over the MAO enzymes, high selectivity over KDM1B and unrivaled subnanomolar cellular activity in differentiation and colony formation assays on mixed lineage leukemia (MLL)-translocated acute myeloid leukemia (AML) cell lines. ORY-1001 provokes a time and dose-dependent induction of the Cd11b differentiation marker in MLL-AF9 cells, which interestingly preceeds changes in H3K4me2 levels. While MLL-translocated cells are especially sensitive, other acute leukemia (AL) cell lines also respond to ORY-1001 trans[1].
In Vivo	ORY-1001 trans reduces AML tumor growth in mice and rat xenografts and increases survival time in a disseminated model of T-ALL[1].
References	[1]. Maes T, et al. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. Epigenomics. 2015;7(4):609-26. doi: 10.2217/epi.15.9.