1. Epigenetics
  2. Histone Demethylase
  3. RN-1 dihydrochloride

RN-1 dihydrochloride 

Cat. No.: HY-110130
Handling Instructions

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.

For research use only. We do not sell to patients.

RN-1 dihydrochloride Chemical Structure

RN-1 dihydrochloride Chemical Structure

CAS No. : 1781835-13-9

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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].

IC50 & Target

IC50: 70 nM (LSD1), 0.51 μM (MAO-A) and 2.785 μM (MAO-B)[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

452.42

Formula

C₂₃H₃₁Cl₂N₃O₂

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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RN-1 dihydrochloride
Cat. No.:
HY-110130
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