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.
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- No. CAS: 133613-71-5
- Fòrmula: C11H14O3
- Peso molecular:194.23
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
Descripciòn
IC50 & Target
[3]|
STAT3 250-500 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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.
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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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No. CAS 133613-71-5
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Appearance Solid
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Peso molecular 194.23
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[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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