Phanginin H
Phanginin H is an Autophagy inducer with an IC50 of 18.13 μM in PANC-1 cells. Phanginin H induces Reactive Oxygen Species accumulation and mitochondrial depolarization, activates AMPK signaling, inhibits mTORC1/ULK signaling and promotes autophagic flux, and simultaneously induces G2/M phase cell cycle arrest, thereby inhibiting PANC-1 cell proliferation, spheroid formation, and migration. Phanginin H can be used in research related to pancreatic ductal adenocarcinoma.
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- CAS No.: 1011528-65-6
- Formule: C21H28O4
- Masse moléculaire:344.44
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
Phanginin H is an Autophagy inducer with an IC50 of 18.13 μM in PANC-1 cells. Phanginin H induces Reactive Oxygen Species accumulation and mitochondrial depolarization, activates AMPK signaling, inhibits mTORC1/ULK signaling and promotes autophagic flux, and simultaneously induces G2/M phase cell cycle arrest, thereby inhibiting PANC-1 cell proliferation, spheroid formation, and migration. Phanginin H can be used in research related to pancreatic ductal adenocarcinoma[1][2][3].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PANC-1 | IC50 |
18.13 μM
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Cytotoxicity against human PANC-1 pancreatic ductal adenocarcinoma cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay.
Cytotoxicity against human PANC-1 pancreatic ductal adenocarcinoma cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay.
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18178229 |
In Vitro
Anti-cancerCell Cycle RegulationAutophagyMitochondrial FunctionOxidative StressOthers
Anti-cancer
Phanginin H (compound 4) (40 μM; 48 h) inhibits the proliferation of PANC-1 cells with an IC50 of 18.13 μM[2].
Phanginin H (5-10 μM; 48 h) significantly inhibits DNA synthesis and cell proliferation in PANC-1 cells[2].
Phanginin H (2.5-10 μM; 24 and 48 h) significantly impairs the migration of PANC-1 cells[2].
Phanginin H (5-10 μM; 24 h) significantly inhibits the invasive capacity of PANC-1 cells[2].
Phanginin H (0.625-10 μM; 24 h) downregulates the expression of cancer stem cell markers (CD44, ALDH1A1, Bmi1) and the EMT marker Vimentin in PANC-1 cells[2].
Phanginin H (compound 11) (20 μM; 48 h) lacks significant cytotoxicity against A2780, HEY, AGS, and A549 cancer cell lines[3].
Phanginin H (5-10 μM; 48 h) significantly inhibits DNA synthesis and cell proliferation in PANC-1 cells[2].
Phanginin H (2.5-10 μM; 24 and 48 h) significantly impairs the migration of PANC-1 cells[2].
Phanginin H (5-10 μM; 24 h) significantly inhibits the invasive capacity of PANC-1 cells[2].
Phanginin H (0.625-10 μM; 24 h) downregulates the expression of cancer stem cell markers (CD44, ALDH1A1, Bmi1) and the EMT marker Vimentin in PANC-1 cells[2].
Phanginin H (compound 11) (20 μM; 48 h) lacks significant cytotoxicity against A2780, HEY, AGS, and A549 cancer cell lines[3].
Cell Cycle Regulation
Autophagy
Phanginin H (1.25-10 μM; 24 h) activates autophagy in PANC-1 cells through the ROS/AMPK/mTORC1 pathway by increasing p-AMPK and decreasing p-mTOR and p-ULK[2].
Phanginin H (5-10 μM; 12 and 24 h) induces a significant increase in autophagic vacuoles in PANC-1 cells[2].
Phanginin H (5-10 μM; 12 and 24 h) activates autophagic flux in PANC-1 cells[2].
Phanginin H (1.25-10 μM; 24 h) increases AMPK Thr172 phosphorylation, decreases mTOR Ser2448 and ULK1 Ser757 phosphorylation, and modulates p62, p-p62, Atg5, and Atg14 in PANC-1 cells, thereby activating ROS/AMPK/mTORC1-related autophagic signaling[2].
Phanginin H (5-10 μM; 12 and 24 h) induces a significant increase in autophagic vacuoles in PANC-1 cells[2].
Phanginin H (5-10 μM; 12 and 24 h) activates autophagic flux in PANC-1 cells[2].
Phanginin H (1.25-10 μM; 24 h) increases AMPK Thr172 phosphorylation, decreases mTOR Ser2448 and ULK1 Ser757 phosphorylation, and modulates p62, p-p62, Atg5, and Atg14 in PANC-1 cells, thereby activating ROS/AMPK/mTORC1-related autophagic signaling[2].
Mitochondrial Function
Oxidative Stress
Phanginin H (5, 10, 20 μM; 24 h) promotes ROS generation in PANC-1 cells[2].
Others
Phanginin H (compound 8) shows no cytotoxic activity against MCF-7, HeLa, HT-29, and KB cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[2]
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Cell Line:PANC-1
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Concentration:5, 10 μM
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Incubation Time:48 h
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Result:Potently inhibited cell proliferation, as demonstrated by a decrease in Click-EdU-488 fluorescence relative to total nuclei.
Cell Cycle Analysis[2]
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Cell Line:PANC-1
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Concentration:1.25, 2.5, 5, 10 μM
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Incubation Time:18 h
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Result:Arrested cells at the G2/M phase.
Western Blot Analysis[2]
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Cell Line:PANC-1
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Concentration:1.25, 2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Increased the expression of Cyclin B1 and decreased the levels of Cyclin D1, cdc25C, and CDK4, while levels of cdc2, p-cdc2 (Thr14/Tyr15), and p21 remained unchanged.\nUp-regulated the phosphorylation level of AMPK (Thr172) and down-regulated phosphorylation of mTOR (Ser2448) and ULK (Ser757).
This was followed by regulation of key autophagy markers, including a decrease in p62, changes in LC3B, an increase in Atg14, and a decrease in Atg5.
Cell Migration Assay [2]
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Cell Line:PANC-1
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Concentration:2.5, 5, 10 μM
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Incubation Time:24 and 48 h
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Result:Significantly impeded the migration in the wound healing assay.
Cell Invasion Assay[2]
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Cell Line:PANC-1
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Concentration:5, 10 μM
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Incubation Time:24 h
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Result:Significantly impeded the invasive ability.
Western Blot Analysis[2]
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Cell Line:PANC-1
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Concentration:0.625, 1.25, 2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Down-regulated the expression levels of cancer stem cell markers CD44, ALDH1A1, and Bmi1, as well as the EMT marker Vimentin.
Cell Cytotoxicity Assay[3]
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Cell Line:A2780, HEY, AGS, A549
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Concentration:20 μM
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Incubation Time:48 h
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Result:Showed no obvious effect on any of the four cell lines up to 20 μM.
Resulted in cell viabilities of 95.4%, 91.7%, 85.8%, and 74.8% in A2780, HEY, AGS, and A549 cells, respectively.
Related Protocols :
- Mitochondrial membrane-potential fluorescent assay
- ROS/oxidative-stress fluorescent staining
- BrdU Incorporation Assay
- Cell migration
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Suspension Spheroid Formation (Low-Adhesion/Forced Aggregation)
- Dye-dilution cell tracking and proliferation staining
- Protocol for Cell Cycle
- CCK-8/WST-8 Cell Proliferation Assay
- Hanging Drop Spheroid Culture
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Flow cytometric DNA-content cell-cycle staining
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Autophagy
- Lysosome and acidic-vesicle live-cell staining
- MTT Cell Proliferation Assay
- Macroautophagy Solutions
Chemical Information
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CAS No. 1011528-65-6
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Masse moléculaire 344.44
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Formule C21H28O4
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SMILES
COC([C@]1([C@@]2([H])[C@]3(CCC1)[C@@]4([H])[C@@](C5=C(C=CO5)[C@@H]([C@]4([H])CC2)C)([H])OC3)C)=O
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Select Batch:
Pureté:
99.98%
Assay:
99.98%
ee.:
99.98%
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Phanginin H Related Classifications
HY-N21627 Related Classifications
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Keywords
- Phanginin H
- 1011528-65-6
- Autophagy
- Reactive Oxygen Species (ROS)
- AMPK
- mTOR
- AMP-activated protein kinase
- Mammalian target of Rapamycin
- reactive oxygen species generation
- mTORC1 activity
- PANC-1 pancreatic ductal adenocarcinoma cells
- phosphorylation of AMPK at Thr172
- mitochondrial depolarization
- autophagy inducer
- ROS/AMPK/mTORC1 pathway
- mTOR phosphorylation at Ser2448
- AMPK signaling pathway
- ULK1 phosphorylation at Ser757
- Inhibitor
- inhibitor
- inhibit