ORY-1001

Modify Date: 2024-01-08 18:37:09

ORY-1001 Structure
ORY-1001 structure
Common Name ORY-1001
CAS Number 1431304-21-0 Molecular Weight 286.375
Density N/A Boiling Point N/A
Molecular Formula C17H22N2O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of ORY-1001


ORY-1001 (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases; exhibits low nanomolar cellular activity (EC50 < 1 nM) in the THP1 differentiation assay and induces the CD11b marker within 6 hr of treatment in FACS based differentiation assay in THP1 cell line; induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML; exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of AML xenograft models.

 Names

Name ORY-1001

 ORY-1001 Biological Activity

Description ORY-1001 (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases; exhibits low nanomolar cellular activity (EC50 < 1 nM) in the THP1 differentiation assay and induces the CD11b marker within 6 hr of treatment in FACS based differentiation assay in THP1 cell line; induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML; exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of AML xenograft models.
References 1. Maes T, et al. Cancer Cell. 2018 Mar 12;33(3):495-511.e12.

 Chemical & Physical Properties

Molecular Formula C17H22N2O2
Molecular Weight 286.375