ORY-1001

ORY-1001 is an inhibitor of lysine-specific demethylase 1 (LSD1), an oxidase that demethylates histone 3 at lysine 4 (H3K4) and H3K9 (IC50 = 0.018 µM). It is selective for LSD1 over LSD2, monoamine oxidase A (MAO-A), and MAO-B (IC50s = >100 µM) but does inhibit spermine oxidase (IC50 = 7.4 µM). ORY-1001 also inhibits the imidazoline I2 receptor, norepinephrine and dopamine transporters, and L-type voltage-gated calcium channels (IC50s = 0.37, 2.4, 1.7, and 4.9 µM, respectively). It induces accumulation of dimethylated H3K4 (H3K4me2) in THP-1 cells (EC50 = 0.0022 µM) and reduces viability in a panel of primary acute myeloid leukemia (AML) cells when used at a concentration of 100 nM. ORY-1001 (0.0125 mg/kg) increases survival in a patient-derived xenograft (PDX) mouse model of T cell acute lymphoblastic leukemia (T-ALL). Formulations containing ORY-1001 have been used in the treatment of AML.Formal Name: rel-N1-[(1R,2S)-2-phenylcyclopropyl]-1,4-cyclohexanediamine, dihydrochloride. CAS Number: 1431326-61-2. Synonyms: Iadademstat, RG-6016. Molecular Formula: C15H22N2 . 2HCl. Formula Weight: 303.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: PBS (pH 7.2): 10 mg/ml. lambdamax: 212, 264 nm. SMILES: NC1CCC(N[C@@H]2C[C@H]2C3=CC=CC=C3)CC1.Cl.Cl. InChi Code: InChI=1S/C15H22N2.2ClH/c16-12-6-8-13(9-7-12)17-15-10-14(15)11-4-2-1-3-5-11,,/h1-5,12-15,17H,6-10,16H2,2*1H/t12?,13?,14-,15+,,/m0../s1. InChi Key: UCINOBZMLCREGM-RNNUGBGQSA-N.