HSF1/AMPK activator 1
HSF1/AMPK activator 1 is a compound that modulates the HSF1/AMPK axis and the TGF-β1/Smad signaling pathway. HSF1/AMPK activator 1 exhibits anti-hepatic fibrosis activity and metabolic stability. HSF1/AMPK activator 1 inhibits fibrosis formation and cell proliferation in activated hepatic stellate cells. HSF1/AMPK activator 1 alleviates liver injury and hepatic fibrosis symptoms in fibrotic mice. HSF1/AMPK activator 1 is applicable to research related to hepatic fibrosis.
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- CAS No.: 2170935-59-6
- 화학식: C24H26O8
- 분자량:442.46
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
24 μM
Compound: 4
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Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay
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[PMID: 28960979] |
In Vitro
HSF1/AMPK activator 1 (Compound 11) (0-20 μM; 48 h) potently inhibits fibronectin expression in human LX-2 cells treated with TGF-β1, with an IC50 of 0.7 μM. At 10 μM for 48 h, it shows an inhibition rate of 91.6 ± 3.8% without associated cytotoxicity[1].
HSF1/AMPK activator 1 (0-80 μM; 48 h) exhibits no cytotoxicity in human LX-2 and HEK-293 cells even at concentrations as high as 80 μM[1].
HSF1/AMPK activator 1 (2.5-10 μM; 48 h) inhibits the proliferation of human LX-2 cells treated with TGF-β1 in a dose-dependent manner[1].
HSF1/AMPK activator 1 (2.5-10 μM; 48 h) dose-dependently reduces the expression of fibronectin, type I collagen and α-smooth muscle actin (α-SMA)-fibrosis markers-at both transcriptional and translational levels in TGF-β1-treated human LX-2 cells[1].
HSF1/AMPK activator 1 (2.5-10 μM; 48 h) inhibits TGF-β1-induced phosphorylation and nuclear translocation of Smad3 in a dose-dependent manner in human LX-2 cells, thereby suppressing the TGF-β1/Smad signaling pathway[1].
HSF1/AMPK activator 1 (2.5-10 μM; 48 h) inhibits proliferation, fibrosis and the TGF-β1/Smad signaling pathway in TGF-β1-treated mouse hepatic stellate cells in a dose-dependent manner[1].
HSF1/AMPK activator 1 (2.5-10 μM; 48 h) dose-dependently activates the HSF1/AMPK metabolic axis in TGF-β1-treated human LX-2 cells and mouse hepatic stellate cells, increases the phosphorylation levels of AMPK and HSF1, and promotes the nuclear localization of activated HSF1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TGF-β1-treated human LX-2 hepatic stellate cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Dose-dependently reversed TGF-β1-induced high proliferation, as indicated by decreased EdU signals.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 8 weeks old, 18-20 g, CCl4-induced liver fibrosis)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.p.; once every other day; 4 weeks
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Result:Decreased liver weight.
Reduced plasma AST and ALT levels.
Lowered liver cleaved caspase-3 signal intensity.
Reduced liver CD68 signal intensity (a marker of hepatic inflammation).
Downregulated hepatic mRNA and protein levels of fibrosis markers fibronectin, collagen I, and α-SMA.
Decreased hepatic Smad3 phosphorylation.
Suppressed liver fiber accumulation as measured by Masson staining and immunofluorescence for α-SMA and fibronectin.
- Collagen: Sirius Red Staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Fibrosis/Collagen Morphometry
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 2170935-59-6
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분자량 442.46
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화학식 C24H26O8
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SMILES
O=C1OC(C)(C2=C[C@H]3[C@]4(C)C5=C([C@H](O[C@]6([C@@]5([C@@](C)(C[C@]4([C@]7(C2=C1)OC7)[H])C(O6)=O)O)[H])C)O3)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HSF1/AMPK activator 1 Related Classifications
HY-181808 Related Classifications
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