1. Epigenetics PI3K/Akt/mTOR TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  2. AMPK TGF-beta/Smad Collagen
  3. 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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HSF1/AMPK activator 1

HSF1/AMPK activator 1 Chemical Structure

CAS No. : 2170935-59-6

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Description

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[1].

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.

Cell Proliferation Assay[1]

Cell Line: TGF-β1-treated human LX-2 hepatic stellate cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 48 h
Result: Dose-dependently reversed TGF-β1-induced high proliferation, as indicated by decreased EdU signals.
In Vivo

HSF1/AMPK activator 1 (compound 11) (10-30 mg/kg; i.p.; once every other day; 4 weeks) significantly ameliorates liver injury, hepatic inflammation, and liver fibrosis in CCl4-treated mice[1].

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

Animal Model: C57BL/6J (male, 8 weeks old, 18-20 g, CCl4-induced liver fibrosis)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.p.; once every other day; 4 weeks
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.
Molecular Weight

442.46

Formula

C24H26O8

CAS No.
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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    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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HSF1/AMPK activator 1
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