Galiellalactone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种小分子直接 STAT3 抑制剂，可抑制 IL-6 诱导的 SEAP 表达，IC50 为 200-500 nM。

A small molecule, direct STAT3 inhibitor that inhibits the IL-6-induced SEAP expression with IC50 of 200-500 nM, blocks the binding of the activated STAT3 dimers to DNA; induces apoptosis of p-Stat3 positive PCa cells, and Stat3-mediated transcription with IC50 of 5 uM, reduces the expression of Bcl-2, Bcl-x(L), c-myc, and cyclin D1; covalently binds to one or more cysteines in STAT3 and inhibits STAT3 binding to DNA and thus blocks STAT3 signaling without affecting phosphorylation; reduces tumor growth and decreases lymph node metastases in mice model of prostate cancer.

Galiellalactone (2.5-25 μM; 24-72 hour) induces apoptosis of prostate cancer (PCa) cell lines expressingp-Stat3.Galiellalactone (2.5-25 μM; 24-72 hour) decreases viability of DU145 cells.Galiellalactone (10 μM) inhibits STAT3 signaling activity as assessed by luciferase reporter gene assay in IL-6-stimulated LNCaP cells.Galiellalactone (10-100 μM; 1 hour) binds directly to STAT3 in DU145 cells .Apoptosis Analysis 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 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 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 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 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.

Galiellalactone (1, 3?mg/kg; daily i.p. for 3 weeks) inhibits PCa tumor growth in vivo. Animal Model:Male nude NMR1 mice are injected PCa cell 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.

Galiellalactone

JAK/STAT Signaling

STAT

STAT

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133613-71-5

194.2

C11H14O3

>98% (HPLC)

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

(7bS)-5,5aR,6,7,7aR,7b-hexahydro-7b-hydroxy-4S-methyl-indeno[1,7-bc]furan-2(4H)-one

(-20℃)

With Ice Pack

≥ 2 years