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Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs). RN-1 is a potent, irreversible inhibitor of LSD1 (IC50 = 70 nM). It is much less effective against MAO-A and MAO-B (IC50s = 0.51 and 2.8 µM, respectively). Following intraperitoneal administration, RN-1 penetrates the blood-brain barrier and distributes in mice to a brain/plasma exposure ratio of 88.9. It blocks long-term but not short-term memory in mice. RN-1 also induces cytotoxicity in ovarian cancer cell lines and induces fetal hemoglobin synthesis while reducing disease pathology in sickle cell mice.Formal Name: rel-1-(4-methyl-1-piperazinyl)-2-[[(1R,2S)-2-[4-(phenylmethoxy)phenyl]cyclopropyl]amino]-ethanone, dihydrochloride. CAS Number: 1781835-13-9. Synonyms: LSD1 Inhibitor IV. Molecular Formula: C23H29N3O2 . 2HCl. Formula Weight: 452.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 0.3 mg/ml, PBS (pH 7.2): 0.5 mg/ml. lambdamax: 228 nm. SMILES: CN1CCN(C(CN[C@@H]2[C@@H](C3=CC=C(OCC4=CC=CC=C4)C=C3)C2)=O)CC1.Cl.Cl. InChi Code: InChI=1S/C23H29N3O2.2ClH/c1-25-11-13-26(14-12-25)23(27)16-24-22-15-21(22)19-7-9-20(10-8-19)28-17-18-5-3-2-4-6-18,,/h2-10,21-22,24H,11-17H2,1H3,2*1H/t21-,22+,,/m1../s1. InChi Key: WMHAFZOOUBPQRX-ZZYOSWMOSA-N.
Keywords:
LSD1 Inhibitor IV, rel-1-(4-methyl-1-piperazinyl)-2-[[(1R,2S)-2-[4-(phenylmethoxy)phenyl]cyclopropyl]amino]-ethanone, dihydrochloride
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