Cas No.: | 1781835-13-9 |
Chemical Name: | RN1, RN 1 |
Synonyms: | RN1, RN 1 |
SMILES: | C1C=C(COC2C=CC([C@@H]3[C@H](NCC(N4CCN(C)CC4)=O)C3)=CC=2)C=CC=1.Cl.Cl |
Formula: | C23H31Cl2N3O2 |
M.Wt: | 452.417 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC50 values of 0.51 μM and 2.785 μM respectively[1][2]. |
In Vivo: | RN-1 (3-10 mg/kg; i.p.; daily; for 2 or 4 consecutive weeks) dihydrochloride effectively induces fetal hemoglobin (HbF) levels in red blood cells and reduces disease pathology in SCD mice[2]. In C57BL/6 male mice, after intraperitoneal administration of RN-1 dihydrochloride (10 mg/kg), concentrations are detectable up to 24 h post dose in both plasma and brain tissues. The brain/plasma exposure ratio is 88.9. RN-1 dihydrochloride significantly impairs long-term memory, but not short-term memory[1]. Animal Model: Sickle cell disease (SCD) mice[2] Dosage: 3 mg/kg or 10 mg/kg Administration: i.p.; daily; for 2 or 4 consecutive weeks Result: Effectively induced HbF levels in red blood cells and reduced disease pathology in SCD mice. |
In Vitro: | RN-1 dihydrochloride shows cytotoxic for ovarian cancer cells (SKOV3, OVCAR3, A2780 and cisplatin-resistant A2780cis), with IC50 values of ≈100-200 μM[3]. |