2. Autophagy Apoptosis
  3. Autophagy Apoptosis
  4. Autophagy-IN-1

Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer.

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Autophagy-IN-1 Chemical Structure

Autophagy-IN-1 Chemical Structure

CAS No. : 3031485-19-2

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Based on 1 publication(s) in Google Scholar

Autophagy-IN-1 Related Antibodies

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Description

Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer[1].

IC50 & Target

Autophagy, Apoptosis[1]
In Vitro

Autophagy-IN-1 (compound 6) (1 and 5 μM; 8 h) induces apoptosis of HCT116 cells concentration-dependently[1].
Autophagy-IN-1 (0.5, 1, 5 and 10 μM; 6 h) decreases pro-PARP1, pro-caspase 8 and pro-caspase 3; increases Cleaved-PARP1, Cleaved-caspase 8 and Cleaved-caspase 3 concentration-dependently[1].
Autophagy-IN-1 increases LC3B-II, p62, and LAMP1 in HCT116 and SW620 cells, and increases number of autophagic/mitophagic vacuoles in HCT116 cells[1].

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

Autophagy-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 1 and 5 μM
Incubation Time: 8 h
Result: Induced 10.11% and 33.52% apoptosis of HCT116 cells at 1 μM and 5 μM.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.5, 1, 5 and 10 μM
Incubation Time: 24 h
Result: Decreased pro-PARP1, pro-caspase 8 and pro-caspase 3; increased Cleaved-PARP1, Cleaved-caspase 8 and Cleaved-caspase 3 concentration-dependently.

Cell Autophagy Assay[1]

Cell Line: HCT116, SW620, and NCM460 cells
Concentration: 0.5, 1, 5 and 10 μM
Incubation Time: 0, 1, 2, 4, 9, 12 and 24 h
Result: Led to a time- and dose-dependent increase of the levels of LC3B-II, p62, and LAMP1 in HCT116 and SW620 cells, and increased number of autophagic/mitophagic vacuoles in HCT116 cells.
In Vivo

Autophagy-IN-1 (50 and 100 mg/kg; IP, daily for 15 days) significantly inhibits tumor growth in an HCT116 xenograft mouse model[1].

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

Animal Model: Male BALB/c nude mice[1]
Dosage: 50 and 100 mg/kg
Administration: IP, daily for 15 days
Result: Significantly inhibited tumor growth and did not observe weight loss.
Molecular Weight

427.45

Formula

C23H25NO7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1O[C@@H](O/C=C([C@@H]2CC3=CC=C4NC(OC(C)(C)C)=O)/C(O[C@H]2C3=C4)=O)C(C)=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (233.95 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 2.3395 mL 11.6973 mL 23.3945 mL
5 mM 0.4679 mL 2.3395 mL 4.6789 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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:
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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).
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. 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 2.3395 mL 11.6973 mL 23.3945 mL 58.4864 mL
5 mM 0.4679 mL 2.3395 mL 4.6789 mL 11.6973 mL
10 mM 0.2339 mL 1.1697 mL 2.3395 mL 5.8486 mL
15 mM 0.1560 mL 0.7798 mL 1.5596 mL 3.8991 mL
20 mM 0.1170 mL 0.5849 mL 1.1697 mL 2.9243 mL
25 mM 0.0936 mL 0.4679 mL 0.9358 mL 2.3395 mL
30 mM 0.0780 mL 0.3899 mL 0.7798 mL 1.9495 mL
40 mM 0.0585 mL 0.2924 mL 0.5849 mL 1.4622 mL
50 mM 0.0468 mL 0.2339 mL 0.4679 mL 1.1697 mL
60 mM 0.0390 mL 0.1950 mL 0.3899 mL 0.9748 mL
80 mM 0.0292 mL 0.1462 mL 0.2924 mL 0.7311 mL
100 mM 0.0234 mL 0.1170 mL 0.2339 mL 0.5849 mL
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Autophagy-IN-1 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:

Autophagy-IN-13031485-19-2AutophagyApoptosisanticancercolorectal cancerHCT116SW620 cellscell cycleBALB/c nude miceautophagosomelysosome fusionInhibitorinhibitorinhibit

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