肉盘菌内酯
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- CAS号:
- 133613-71-5
- 英文名:
- galiellalactone
- 英文别名:
- galiellalactone;SOIISBQQYAGDKM-QJSROADHSA-N;(4S,5aR,7aR,7bS)-5,5a,6,7,7a,7b-Hexahydro-7b-hydroxy-4-methylindeno[1,7-bc]furan-2(4H)-one;Indeno[1,7-bc]furan-2(4H)-one, 5,5a,6,7,7a,7b-hexahydro-7b-hydroxy-4-methyl-, (4S,5aR,7aR,7bS)-
- 中文名:
- 肉盘菌内酯
- 中文别名:
- 伽利略内酯;半乳糖内酯;肉盘菌内酯;化合物 T22796
- CBNumber:
- CB21397587
- 分子式:
- C11H14O3
- 分子量:
- 194.23
- MOL File:
- 133613-71-5.mol
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肉盘菌内酯化学性质
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沸点:
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400.7±38.0 °C(Predicted)
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密度:
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1.29±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO:0.97(Max Conc. mg/mL);4.99(Max Conc. mM)
Ethanol:0.97(Max Conc. mg/mL);4.99(Max Conc. mM)-
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形态:
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White to light tan solid.
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酸度系数(pKa):
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12.48±0.40(Predicted)
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肉盘菌内酯性质、用途与生产工艺
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。
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STAT3
250-500 nM (IC
50
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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 .
Galiellalactone (5-50 μM; 1 hour) interferes with STAT3 DNA binding without inhibiting phosphorylation in DU145 cells .
Apoptosis Analysis
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Cell Line:
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DU145, PC-3, and LNCaP cells
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Concentration:
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0, 2.5, 5, 10, 25 μM
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Incubation Time:
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24, 48, 72 hours
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Result:
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Induced an apoptotic response in PC-3 and DU145 cells.
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Cell Viability Assay
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Cell Line:
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DU145 cells
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Concentration:
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0, 2.5, 5, 10, 17.5, 25 μM
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Incubation Time:
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24, 48, 72 hours
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Result:
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Decreased DU145 cells viability in a dose- and time-dependent manner.
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Western Blot Analysis
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Cell Line:
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DU145 cells
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Concentration:
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0, 10, 25 μM
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Incubation Time:
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48 hours
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Result:
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Induced expression of the apoptotic marker cleaved caspase-3 and increased expression of cleaved PARP.
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Western Blot Analysis
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Cell Line:
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DU145 cells
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Concentration:
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0, 10, 25, 50, 100 μM
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Incubation Time:
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1 hour
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Result:
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Prevented the binding of the biotinylated analogue of galiellalactone (GL-biot) to STAT3 in a dose-dependent manner demonstrating competitive binding.
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Western Blot Analysis
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Cell Line:
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DU145 cells
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Concentration:
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0, 5, 10, 25, 50 μM
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Incubation Time:
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1 hour
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Result:
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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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Galiellalactone (1, 3 mg/kg; daily i.p. for 3 weeks) inhibits PCa tumor growth in vivo.
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Animal Model:
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Male nude NMR1 mice are injected PCa cell
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Dosage:
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0, 1, 3 mg/kg
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Administration:
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Daily i.p. injections for 3 weeks
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Result:
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Reduced the tumor growth rate in DU145 xenografts by 41-42% and was well tolerated.
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肉盘菌内酯
上下游产品信息
上游原料
下游产品
133613-71-5, 肉盘菌内酯 相关搜索:
- 微生物代谢物
- 化合物 T22796
- 伽利略内酯
- 半乳糖内酯
- 肉盘菌内酯
- 133613-71-5
- Indeno[1,7-bc]furan-2(4H)-one, 5,5a,6,7,7a,7b-hexahydro-7b-hydroxy-4-methyl-, (4S,5aR,7aR,7bS)-
- (4S,5aR,7aR,7bS)-5,5a,6,7,7a,7b-Hexahydro-7b-hydroxy-4-methylindeno[1,7-bc]furan-2(4H)-one
- SOIISBQQYAGDKM-QJSROADHSA-N
- galiellalactone