1. Autophagy Apoptosis
  2. Autophagy Apoptosis
  3. 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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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.

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.
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

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

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    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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Autophagy-IN-1
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