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。
| 生物活性 | Galiellalactone is a is a small non-toxic and non-mutagenicfungalmetabolite, a selective inhibitor ofSTAT3signaling, with anIC50of 250-500 nM. Galiellalactone can be used to research castration-resistant prostatecancer[1][2][3]. |
| IC50& Target[3] | |
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].
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].
| 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. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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