Aspulvinone O
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Aspulvinone O is a selective inhibitor of glutamate oxaloacetate aminotransferase GOT1. Aspulvinone O inhibits glutamine metabolism and reduces NADPH production, thereby inducing oxidative stress and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cells. Aspulvinone O inhibits PDAC cell proliferation in vitro and tumor growth in xenograft models.
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- Pureté: 96.0%
- CAS No.: 914071-54-8
- Formule: C27H28O6
- Masse moléculaire:448.51
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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GOT/AST |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| J774.1 | IC50 |
3 μM
Compound: 11
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Anti-inflammatory activity against mouse J774A.1 macrophage assessed as reduction in LPS-induced LDH release incubated for 1 hr in presence of nigericin by LDH assay
Anti-inflammatory activity against mouse J774A.1 macrophage assessed as reduction in LPS-induced LDH release incubated for 1 hr in presence of nigericin by LDH assay
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[PMID: 35293744] |
Aspulvinone O (0.1-100 μM; 48 h) inhibits the proliferation of pancreatic ductal adenocarcinoma cell lines (SW1990, PANC-1, AsPC-1) with IC50 of 20.54-26.80 μM, showing selectivity for cancer cells over normal cells[1].
Aspulvinone O (10-40 μM; 48 h) arrests the cell cycle of SW1990 cells at the S phase and induces apoptosis[1].
Aspulvinone O (10-40 μM; 24 h) reduces the levels of glutamine metabolic intermediates (OAA, malate) and the NADPH/NADP+ ratio[1] in SW1990 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW1990, PANC-1, AsPC-1 (human PDAC cells)
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Concentration:0.1-100 μM
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Incubation Time:48 h
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Result:Dose-dependent growth inhibition with IC50 of 20.54 μM (SW1990), 26.80 μM (PANC-1), and 23.12 μM (AsPC-1), respectively, while showed no significant cytotoxicity (IC50 >100 μM) against normal HPDE6C7 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17/scid male mice (8 weeks old, ~20 g), SW1990 cell-derived xenograft model[1]
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Dosage:2.5 mg/kg, 5 mg/kg
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Administration:Intraperitoneal injection (i.p.), daily for 14 days, starting when tumors reached ~3 mm diameter
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Result:Significantly reduced tumor volume and weight compared to control. Showed a 60% reduction in tumor weight in the 5 mg/kg group, at day 14 and a 55% reduction in tumor volume.
Decreased levels of oxaloacetate (OAA) and malate (~50% reduction), increased aspartate (Asp) and glutamine (Gln) (~30% increase), and a 45% decrease in NADPH/NADP+ ratio compared to control.
No significant changes in body weight or histomorphology, indicating good tolerability.
Chemical Information
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CAS No. 914071-54-8
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Appearance Solid
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Masse moléculaire 448.51
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Formule C27H28O6
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Color Light yellow to brown
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SMILES
OC1=C(C2=CC(C/C=C(C)/C)=C(O)C=C2O)C(O/C1=C/C3=CC(C/C=C(C)/C)=C(O)C=C3)=O
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Structure Classification
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Initial Source
Aspergillus terreus
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 25 mg/mL (55.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Sun W, et al. Aspulvinone O, a natural inhibitor of GOT1 suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism. Cell Commun Signal. 2019;17(1):111. [Content Brief]
[2]. Yan S, et al. Discovery of GOT1 Inhibitors from a Marine-Derived Aspergillus terreus That Act against Pancreatic Ductal Adenocarcinoma. Mar Drugs. 2021 Oct 20;19(11):588. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2296 mL | 11.1480 mL | 22.2960 mL | 55.7401 mL |
| 5 mM | 0.4459 mL | 2.2296 mL | 4.4592 mL | 11.1480 mL | |
| 10 mM | 0.2230 mL | 1.1148 mL | 2.2296 mL | 5.5740 mL | |
| 15 mM | 0.1486 mL | 0.7432 mL | 1.4864 mL | 3.7160 mL | |
| 20 mM | 0.1115 mL | 0.5574 mL | 1.1148 mL | 2.7870 mL | |
| 25 mM | 0.0892 mL | 0.4459 mL | 0.8918 mL | 2.2296 mL | |
| 30 mM | 0.0743 mL | 0.3716 mL | 0.7432 mL | 1.8580 mL | |
| 40 mM | 0.0557 mL | 0.2787 mL | 0.5574 mL | 1.3935 mL | |
| 50 mM | 0.0446 mL | 0.2230 mL | 0.4459 mL | 1.1148 mL |
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