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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

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Galiellalactone Chemical Structure

CAS No.: 133613-71-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[3]

STAT3

250-500 nM (IC₅₀)

All STAT Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BT-549	IC₅₀	12.68 μM Compound: 1	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	[PMID: 28705432]
DU-145	IC₅₀	3.02 μM Compound: 1	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	[PMID: 27111731]
MDA-MB-231	IC₅₀	16.93 μM Compound: 1	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	[PMID: 28705432]
MDA-MB-468	IC₅₀	17.48 μM Compound: 1	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	[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.

Apoptosis Analysis^[1]

Cell Line:

DU145, PC-3, and LNCaP cells
Concentration:

0, 2.5, 5, 10, 25 μM
Incubation Time:

24, 48, 72 hours
Result:

Induced an apoptotic response in PC-3 and DU145 cells.

Cell Viability Assay^[1]

Cell Line:

DU145 cells
Concentration:

0, 2.5, 5, 10, 17.5, 25 μM
Incubation Time:

24, 48, 72 hours
Result:

Decreased DU145 cells viability in a dose- and time-dependent manner.

Western Blot Analysis^[1]

Cell Line:

DU145 cells
Concentration:

0, 10, 25 μM
Incubation Time:

48 hours
Result:

Induced expression of the apoptotic marker cleaved caspase-3 and increased expression of cleaved PARP.

Western Blot Analysis^[2]

Cell Line:

DU145 cells
Concentration:

0, 10, 25, 50, 100 μM
Incubation Time:

1 hour
Result:

Prevented the binding of the biotinylated analogue of galiellalactone (GL-biot) to STAT3 in a dose-dependent manner demonstrating competitive binding.

Western Blot Analysis^[2]

Cell Line:

DU145 cells
Concentration:

0, 5, 10, 25, 50 μM
Incubation Time:

1 hour
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

Galiellalactone (1, 3 mg/kg; daily i.p. for 3 weeks) inhibits PCa tumor growth in vivo^[1].

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

Animal Model:

Male nude NMR1 mice are injected PCa cell^[1]
Dosage:

0, 1, 3 mg/kg
Administration:

Daily i.p. injections for 3 weeks
Result:

Reduced the tumor growth rate in DU145 xenografts by 41-42% and was well tolerated.

Chemical Information

CAS No. 133613-71-5
Appearance Solid
Molecular Weight 194.23
Formula C₁₁H₁₄O₃
Color White to off-white
SMILES

O=C1C2=C[C@@H](C)C[C@@]3([H])CC[C@@]([C@@]23O)([H])O1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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