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Galiellalactone
Galiellalactone 是一种小的无毒且无致突变性的真菌代谢产物，是一种选择性的 STAT3 信号抑制剂，IC50 值为 250-500 nM。Galiellalactone 可用于研究去势抵抗性前列腺癌。
Galiellalactone Chemical Structure
CAS No. : 133613-71-5
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
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].
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| IC50 & Target[3] |
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体外研究
(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].
上海金畔生物科技有限公司 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. |
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体内研究
(In Vivo) |
Galiellalactone (1, 3 mg/kg; daily i.p. for 3 weeks) inhibits PCa tumor growth in vivo[1].
上海金畔生物科技有限公司 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. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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.
[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.
[3]. Weidler M, et, al. Inhibition of interleukin-6 signaling by galiellalactone. FEBS Lett. 2000 Oct 27; 484(1): 1-6.
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