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ORY-1001

Chemical Structure : ORY-1001

CAS No.: 1431326-61-2

ORY-1001 (Iadademstat;RG 6016;RG6016;RG-6016;ORY1001;ORY 1001)

Catalog No.: PC-43206Not For Human Use, Lab Use Only.

ORY-1001 (RG-6016) 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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ORY-1001 (RG-6016, Iadademstat) 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.
ORY-1001 (RG-6016, Iadademstat)  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.
ORY-1001 (RG-6016, Iadademstat)  induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML.
ORY-1001 (RG-6016, Iadademstat)  exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of AML xenograft models.

Physicochemical Properties

M.Wt 303.2704
Formula C15H24Cl2N2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: < 6.8 mg/mL

Chemical Name/SMILES

trans-N1-(2-Phenylcyclopropyl)cyclohexane-1,4-diamine dihydrochloride

References

1. Maes T, et al. Cancer Cell. 2018 Mar 12;33(3):495-511.e12.

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