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RN-1 Hydrochloride

  Cat. No.:  DC7636   Featured
Chemical Structure
1781835-13-9
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Field of application
RN-1 is an inhibitor of lysine specific demethylase 1 (LSD1); exhibits selectivity for LSD1 over monoamine oxidase (MAO)-A and MAO-B (IC50 values are 70 nM, 0.51 and 2.79 μM respectively.
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC11703 T-3775440 hydrochloride T-3775440 hydrochloride is a novel potent, selecitve, irreversible LSD1 inhibitor with IC50 of 2.1 nM.
DC11400 Seclidemstat(SP-2577) Seclidemstat(SP-2577) is a potent LSD1 inhibitor, with a mean IC50 of 127 nM.
DC7636 RN-1 Hydrochloride RN-1 is an inhibitor of lysine specific demethylase 1 (LSD1); exhibits selectivity for LSD1 over monoamine oxidase (MAO)-A and MAO-B (IC50 values are 70 nM, 0.51 and 2.79 μM respectively.
DC5204 OG-L002 OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.
DC7740 ML-324 ML-324 is a JMJD2 histone demethylase inhibitor (JMJD2 IC50 = 920 nM)
DC11106 Vafidemstat (ORY-2001) Vafidemstat (ORY-2001) is an oral, brain penetrant drug that inhibits LSD1 and MAOB by reducing cognitive impairment, including memory loss and neuroinflammation. It also has neuroprotective effects.
DC10586 KDM4D-IN-1 KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
DC7614 IOX1 IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.
DC8491 GSK2879552 GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
DC8385 Disodium (R)-2-Hydroxyglutarate Disodium (R)-2-Hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with Ki of 0.628 mM.
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