Galiellalactone
Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC50 of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer.
For research use only. We do not sell to patients.
- CAS No.: 133613-71-5
- Formula: C11H14O3
- Molecular Weight:194.23
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[3]|
STAT3 250-500 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| BT-549 | IC50 |
12.68 μM
Compound: 1
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Cytotoxic activity against human BT549 cells incubated for 24 hrs by MTT assay
Cytotoxic activity against human BT549 cells incubated for 24 hrs by MTT assay
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[PMID: 28705432] |
| DU-145 | IC50 |
3.02 μM
Compound: 1
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Antiproliferative activity against human DU145 cells after 72 hrs by WST-1 proliferation assay
Antiproliferative activity against human DU145 cells after 72 hrs by WST-1 proliferation assay
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[PMID: 27111731] |
| MDA-MB-231 | IC50 |
16.93 μM
Compound: 1
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Cytotoxic activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay
Cytotoxic activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay
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[PMID: 28705432] |
| MDA-MB-468 | IC50 |
17.48 μM
Compound: 1
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Cytotoxic activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay
Cytotoxic activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay
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[PMID: 28705432] |
In Vitro
Galiellalactone (2.5-25 μM; 24-72 hour) induces apoptosis of prostate cancer (PCa) cell lines expressingp-Stat3[1].
Galiellalactone (2.5-25 μM; 24-72 hour) decreases viability of DU145 cells[1].
Galiellalactone (10 μM) inhibits STAT3 signaling activity as assessed by luciferase reporter gene assay in IL-6-stimulated LNCaP cells[2].
Galiellalactone (10-100 μM; 1 hour) binds directly to STAT3 in DU145 cells [2].
Galiellalactone (5-50 μM; 1 hour) interferes with STAT3 DNA binding without inhibiting phosphorylation in DU145 cells [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:DU145, PC-3, and LNCaP cells
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Concentration:0, 2.5, 5, 10, 25 μM
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Incubation Time:24, 48, 72 hours
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Result:Induced an apoptotic response in PC-3 and DU145 cells.
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Cell Line:DU145 cells
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Concentration:0, 2.5, 5, 10, 17.5, 25 μM
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Incubation Time:24, 48, 72 hours
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Result:Decreased DU145 cells viability in a dose- and time-dependent manner.
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Cell Line:DU145 cells
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Concentration:0, 10, 25 μM
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Incubation Time:48 hours
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Result:Induced expression of the apoptotic marker cleaved caspase-3 and increased expression of cleaved PARP.
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Cell Line:DU145 cells
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Concentration:0, 10, 25, 50, 100 μM
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Incubation Time:1 hour
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Result:Prevented the binding of the biotinylated analogue of galiellalactone (GL-biot) to STAT3 in a dose-dependent manner demonstrating competitive binding.
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Cell Line:DU145 cells
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Concentration:0, 5, 10, 25, 50 μM
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Incubation Time:1 hour
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Result:Inhibited STAT3 binding to DNA in a dose-dependent manner.
Did not affect phosphorylation of STAT3 Tyr-705 and Ser-727 or the expression of total STAT3.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male nude NMR1 mice are injected PCa cell[1]
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Dosage:0, 1, 3 mg/kg
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Administration:Daily i.p. injections for 3 weeks
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Result:Reduced the tumor growth rate in DU145 xenografts by 41-42% and was well tolerated.
Chemical Information
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CAS No. 133613-71-5
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Appearance Solid
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Molecular Weight 194.23
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Formula C11H14O3
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Color White to off-white
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SMILES
O=C1C2=C[C@@H](C)C[C@@]3([H])CC[C@@]([C@@]23O)([H])O1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hellsten R, et, al. Galiellalactone is a novel therapeutic candidate against hormone-refractory prostate cancer expressing activated Stat3. Prostate. 2008 Feb 15; 68(3): 269-80. [Content Brief]
[2]. Doncow DN, et, al. Galiellalactone is a direct inhibitor of the transcription factor STAT3 in prostate cancer cells. J Biol Chem. 2014 Jun 6; 289(23): 15969-78. [Content Brief]
[3]. Weidler M, et, al. Inhibition of interleukin-6 signaling by galiellalactone. FEBS Lett. 2000 Oct 27; 484(1): 1-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Galiellalactone Related Classifications
HY-125170 Related Classifications
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