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

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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Based on 1 publication(s) in Google Scholar

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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].

MedChemExpress (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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(C)CC1)CN[C@@H]2[C@@H](C3=CC=C(OCC4=CC=CC=C4)C=C3)C2.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 20 mg/mL (44.21 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2103 mL 11.0517 mL 22.1034 mL
5 mM 0.4421 mL 2.2103 mL 4.4207 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 20 mg/mL (44.21 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.2103 mL 11.0517 mL 22.1034 mL 55.2584 mL
5 mM 0.4421 mL 2.2103 mL 4.4207 mL 11.0517 mL
10 mM 0.2210 mL 1.1052 mL 2.2103 mL 5.5258 mL
15 mM 0.1474 mL 0.7368 mL 1.4736 mL 3.6839 mL
20 mM 0.1105 mL 0.5526 mL 1.1052 mL 2.7629 mL
25 mM 0.0884 mL 0.4421 mL 0.8841 mL 2.2103 mL
30 mM 0.0737 mL 0.3684 mL 0.7368 mL 1.8419 mL
40 mM 0.0553 mL 0.2763 mL 0.5526 mL 1.3815 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
RN-1 dihydrochloride
Cat. No.:
HY-110130
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