Pseurotin A
Based on 1 Customer Validation
Pseurotin A is a secondary metabolite of Aspergillus and other fungi. Pseurotin A is a competitive inhibitor of chitin synthase and a neuritogenic agent. Pseurotin A inhibits IgE production (IC50 = 3.6 μM). Pseurotin A inhibits the PCSK9-LDLr interaction. Pseurotin A shows dose-dependent reduction of PCSK9, along with increased LDLR levels in hormone-dependent breast cancer cell lines. Pseurotin A exhibits antitumor activity.
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- Pureté : 98%
- CAS No.: 58523-30-1
- Formule: C22H25NO8
- Masse moléculaire:431.44
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Stockage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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Microbial Metabolite |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
>10 nM
Compound: 1
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Cytotoxicity against human K562 cells
Cytotoxicity against human K562 cells
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[PMID: 19179074] |
| K562 | IC50 |
41 μM
Compound: 5
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Cytotoxicity against human K562 cells after 48 hrs by MTT assay
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
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[PMID: 19256529] |
| Lymphocyte | IC50 |
>10 μM
Compound: 1
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Immunosuppressive activity in rat lymphocytes assessed as inhibition of mixed-lymphocyte reaction
Immunosuppressive activity in rat lymphocytes assessed as inhibition of mixed-lymphocyte reaction
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[PMID: 19179074] |
| RAW264.7 | IC50 |
>100 μM
Compound: pseurotin A
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Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production compound treated prior to LPS challenge by Griess assay
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production compound treated prior to LPS challenge by Griess assay
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[PMID: 27976895] |
| Vero | IC50 |
50 μM
Compound: 22
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Antiviral activity against HSV1 F infected in african green monkey Vero cells assessed as reduction of virus-induced cytopathic effect by cellular replication assay
Antiviral activity against HSV1 F infected in african green monkey Vero cells assessed as reduction of virus-induced cytopathic effect by cellular replication assay
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[PMID: 12828470] |
In Vitro
Pseurotin A inhibits the expression of PCSK9 in HepG2 cells, with an IC50 value of 1.2 μM[3].
Pseurotin A (25-100 μM; 72 hours) significantly suppresses the PCSK9 level in a dose dependent manner in BT-474 and T47D BC cell lines[3].
Pseurotin A (25-100 μM; 72 hours) significantly increases LDLR level in a dose dependent manner[3].
Pseurotin A (40-200 μM; 24-72 hours) shows anti-proliferative activity in the hormone-dependent BC cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:BT-474 cells, T47D cells
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Concentration:40-200 μM
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Incubation Time:24-72 hours
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Result:Showed weak but time and dose-dependent inhibition of the growth of BT-474 and T47D BC cells, with gradual decrease of the IC50 values over time (260.83-93.64 μM and 267.84-113.08 μM, respectively).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HFD-fed orthotopic athymic mice (bearing BT-474 tumor cells xenograft mode)[1]
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Dosage:10 mg/kg
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Administration:P.o.; 7X/week, 30 days
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Result:Significantly suppressed the growth of BT474 tumors.
Chemical Information
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CAS No. 58523-30-1
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Appearance Solid
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Masse moléculaire 431.44
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Formule C22H25NO8
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Color White to off-white
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SMILES
O=C1C(C)=C([C@@H](O)[C@@H](O)/C=C\CC)O[C@]12C(N[C@@](OC)(C(C3=CC=CC=C3)=O)[C@@H]2O)=O
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Structure Classification
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Initial Source
Ascomycetes
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Pureté et documentation
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Fiche technique (288 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]. Ishikawa M, et al. Pseurotin A and its analogues as inhibitors of immunoglobulin E [correction of immunoglobuline E] production. Bioorg Med Chem Lett. 2009;19(5):1457-1460. [Content Brief]
[2]. Maiya S, Grundmann A, Li X, Li SM, Turner G. Identification of a hybrid PKS/NRPS required for pseurotin A biosynthesis in the human pathogen Aspergillus fumigatus. Chembiochem. 2007;8(14):1736-1743. [Content Brief]
[3]. Abdelwahed KS, et al. Pseurotin A as a novel suppressor of hormone dependent breast cancer progression and recurrence by inhibiting PCSK9 secretion and interaction with LDL receptor. Pharmacol Res. 2020;158:104847. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pseurotin A Related Classifications
HY-125916 Related Classifications
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