2. Autophagy Apoptosis
  3. Autophagy Apoptosis
  4. ARN5187 trihydrochloride

ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis.

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ARN5187 trihydrochloride Chemical Structure

ARN5187 trihydrochloride Chemical Structure

CAS No. : 1700693-96-4

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Based on 1 publication(s) in Google Scholar

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ARN5187 trihydrochloride Related Antibodies

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Description

ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis[1][2].

IC50 & Target

REV-ERBβ[1]
In Vitro

ARN5187 trihydrochloride (compound 1) (0-100 µM; 48 h) shows cytotoxicity with EC50 of 23.5 µM in BT-474 cells and IC50 of 30.14 µM, >100 µM for BT-474 and HMEC cells, respectively[1][2].
ARN5187 trihydrochloride (0-100 µM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells[1].
ARN5187 trihydrochloride (25, 50 µM) is a lysosomotropic-independent REV-ERB antagonistic activity[1].
ARN5187 trihydrochloride (50 µM; 24 h) shows autophagy inhibition[1].
ARN5187 trihydrochloride (50 µM; 2, 8, 24 h) effects autophagy formation and maturation[1].

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

ARN5187 trihydrochloride Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: BT-474 cells
Concentration: 0-100 µM
Incubation Time: 48 h
Result: Showed cytotoxicity with EC50 of 23.5 µM.

Western Blot Analysis[1]

Cell Line: BT-474 cells
Concentration: 50 µM
Incubation Time: 24 h
Result: Significantly increased the expression of α-LC3-II, α-p62, α-Cleaved PARP.

RT-PCR[1]

Cell Line: BT-474 cells
Concentration: 25, 50 µM
Incubation Time:
Result: Significantly enhanced the expression of BMAL1, PER1 and PEPCK in a dose-dependent manner.
Molecular Weight

506.91

Formula

C24H35Cl3FN3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(CNC2(C3=CC=CC=C3F)CCCC2)C=C1CN4CCN(C)CC4.Cl[H].Cl[H].Cl[H]
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: 

DMSO : 100 mg/mL (197.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9727 mL 9.8637 mL 19.7274 mL
5 mM 0.3945 mL 1.9727 mL 3.9455 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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
DMSO 1 mM 1.9727 mL 9.8637 mL 19.7274 mL 49.3184 mL
5 mM 0.3945 mL 1.9727 mL 3.9455 mL 9.8637 mL
10 mM 0.1973 mL 0.9864 mL 1.9727 mL 4.9318 mL
15 mM 0.1315 mL 0.6576 mL 1.3152 mL 3.2879 mL
20 mM 0.0986 mL 0.4932 mL 0.9864 mL 2.4659 mL
25 mM 0.0789 mL 0.3945 mL 0.7891 mL 1.9727 mL
30 mM 0.0658 mL 0.3288 mL 0.6576 mL 1.6439 mL
40 mM 0.0493 mL 0.2466 mL 0.4932 mL 1.2330 mL
50 mM 0.0395 mL 0.1973 mL 0.3945 mL 0.9864 mL
60 mM 0.0329 mL 0.1644 mL 0.3288 mL 0.8220 mL
80 mM 0.0247 mL 0.1233 mL 0.2466 mL 0.6165 mL
100 mM 0.0197 mL 0.0986 mL 0.1973 mL 0.4932 mL
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ARN5187 trihydrochloride Related Classifications

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.

Keywords:

ARN5187 trihydrochloride1700693-96-4AutophagyApoptosisapoptosisBT-474 cellslysosomotropicchloroquineanticancerα-p62HEK-293 cellsInhibitorinhibitorinhibit

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