ORY-1001 is a KDM1A inhibitor (IC50<20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers (EC50 me2H3K4 and FACS CD11b<1nM). ORY-1001 induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells (EC50<1nM). ORY-1001 does not inhibit non-related histone modifiers.

1431304-21-0

C15H22N2

230.35

ORY 1001;ORY-1001;ORY1001;RG 6016;RG6016;RG-6016;ORY-1001 free base

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years