Galiellalactone
Modify Date: 2024-01-12 18:11:44
Galiellalactone structure
|
Common Name | Galiellalactone | ||
|---|---|---|---|---|
| CAS Number | 133613-71-5 | Molecular Weight | 194.227 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 400.7±38.0 °C at 760 mmHg | |
| Molecular Formula | C11H14O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 182.1±19.5 °C | |
Use of GaliellalactoneGaliellalactone 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]. |
| Name | Galiellalactone |
|---|---|
| Synonym | More Synonyms |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 400.7±38.0 °C at 760 mmHg |
| Molecular Formula | C11H14O3 |
| Molecular Weight | 194.227 |
| Flash Point | 182.1±19.5 °C |
| Exact Mass | 194.094299 |
| PSA | 46.53000 |
| LogP | 0.88 |
| Vapour Pressure | 0.0±2.1 mmHg at 25°C |
| Index of Refraction | 1.577 |
| Indeno[1,7-bc]furan-2(4H)-one, 5,5a,6,7,7a,7b-hexahydro-7b-hydroxy-4-methyl- |
| (4R,5aS,7aS,7bR)-5,5a,6,7,7a,7b-hexahydro-7b-hydroxy-4-methyl-indeno[1,7-bc]furan-2(4H)-one |
| (-)-galiellalactone |
| 7b-Hydroxy-4-methyl-5,5a,6,7,7a,7b-hexahydroindeno[1,7-bc]furan-2(4H)-one |