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  3. Galiellalactone

Galiellalactone 

Cat. No.: HY-125170
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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.

Galiellalactone Chemical Structure

Galiellalactone Chemical Structure

CAS No. : 133613-71-5

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Description

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[1][2][3].

IC50 & Target[3]

STAT3

250-500 nM (IC50)

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].

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].

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.
Molecular Weight

194.23

Formula

C₁₁H₁₄O₃

CAS No.

133613-71-5

SMILES
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

GaliellalactoneSTATNon-toxicnon-mutagenicfungalmetaboliteSTAT3signalingcancerInhibitorinhibitorinhibit

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