ORY-1001 dihydrochloride

Research use only, not for human use.

ORY-1001 dihydrochloride (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM.

ORY-1001 dihydrochloride (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.Blood Cancer Phase 2 Clinical

Ladademstat;RG-6016

Chromatin/Epigenetic

Histone Demethylase

Histone Demethylase

Cancer

——

1431303-72-8

303.27

C15H24Cl2N2

>98% (HPLC)

H2O : 57.75 mg/mL 190.42 mM; DMSO : 0.69 mg/mL 2.28 mM

N[C@@H]1CC[C@@H](N[C@H]2[C@H](C3=CC=CC=C3)C2)CC1.[H]Cl.[H]Cl

(1r,4R)-N1-((1R,2S)-2-phenylcyclopropyl)cyclohexane-1,4-diamine dihydrochloride

(-20℃)

With Ice Pack

≥ 2 years