1. Anti-infection Autophagy
  2. Filovirus Parasite Autophagy
  3. Retro-2

Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is an ebolavirus (EBOV) infection inhibitor with an EC50 of 12.2 µM in HeLa cells. Retro-2 induces cell autophagy.

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Retro-2 Chemical Structure

Retro-2 Chemical Structure

CAS No. : 1201652-50-7

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Based on 1 publication(s) in Google Scholar

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Description

Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is an ebolavirus (EBOV) infection inhibitor with an EC50 of 12.2 µM in HeLa cells. Retro-2 induces cell autophagy[1][2][3].

IC50 & Target

EC50: 12.2 µM (Ebolavirus)[3]

In Vitro

Retro-2 (1 μM; 1-4 hours) induces autophagy in GFP-LC3-expressing HeLa cells and promoted the dramatic cytoplasmic accumulation of large autophagosomes[2].
Retro-2 (1 μM; 0.5-4 hours) treatment hows an increase over time of the abundance of LC3-II protein in cells[2].
Retro-2 impairs the trafficking between autophagosomes and lysosomes. Retro-2 abolishes autolysosomes formation[2].
Retro-2 (20 μM; pretreatment for 30 min) inhibits HeLa cell intoxication by ricin, Shiga-like toxins 1 (Stx1) and 2 (Stx2)[1].
Retro-2 blocked invasion of cells by the intracellular parasite Leishmania, as well as replication of non-enveloped viruses, including polyoma-, papilloma-, and adeno-associated viruses[3].

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

Cell Autophagy Assay[2]

Cell Line: HeLa cells
Concentration: 1 μM
Incubation Time: 1 hour, 2 hours, 4 hours
Result: Resulted in a large significant increase in the number of small and large vesicles.

Western Blot Analysis[2]

Cell Line: HeLa cells
Concentration: 1 μM
Incubation Time: 0.5 hour, 2 hours, 4 hours
Result: Showed an increase over time of the abundance of LC3-II protein in cells.
In Vivo

Retro-2 (2-200 mg/kg; i.p; daily; for 21 days) treatment clearly protects from lethal nasal exposure to ricin in mice. 200 mg/kg of Retro-2 fully protects mice against ricin challenge[1].

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

Animal Model: Female Balb/c mice (Pathogen-free 6-week-old) injected with ricin (2 μg/kg)[1]
Dosage: 2 mg/kg, 10 mg/kg, 20 mg/kg, 200 mg/kg
Administration: Intraperitoneal injection; daily; for 21 days
Result: Protected mice against ricin challenge.
Molecular Weight

320.41

Formula

C19H16N2OS

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(NC1=CC=CC=C1)C2=CC=CC=C2/N=C/C3=CC=C(C)S3.[(E)]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (780.25 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 3.1210 mL 15.6050 mL 31.2100 mL
5 mM 0.6242 mL 3.1210 mL 6.2420 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 (protect from light). 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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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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V2

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: 2.08 mg/mL (6.49 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (6.49 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
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 (protect from light)

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 (protect from light). 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 3.1210 mL 15.6050 mL 31.2100 mL 78.0250 mL
5 mM 0.6242 mL 3.1210 mL 6.2420 mL 15.6050 mL
10 mM 0.3121 mL 1.5605 mL 3.1210 mL 7.8025 mL
15 mM 0.2081 mL 1.0403 mL 2.0807 mL 5.2017 mL
20 mM 0.1561 mL 0.7803 mL 1.5605 mL 3.9013 mL
25 mM 0.1248 mL 0.6242 mL 1.2484 mL 3.1210 mL
30 mM 0.1040 mL 0.5202 mL 1.0403 mL 2.6008 mL
40 mM 0.0780 mL 0.3901 mL 0.7803 mL 1.9506 mL
50 mM 0.0624 mL 0.3121 mL 0.6242 mL 1.5605 mL
60 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3004 mL
80 mM 0.0390 mL 0.1951 mL 0.3901 mL 0.9753 mL
100 mM 0.0312 mL 0.1561 mL 0.3121 mL 0.7803 mL
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Retro-2 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.

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