Penitrem E
Penitrem E is an indole diterpenoid alkaloid with antitumor activity, isolated and extracted from Penicillium commune. Penitrem E is a BK channel antagonist. Penitrem E exerts its antagonistic effect by forming hydrogen bonds with the calcium-binding site of the BK channel, thereby upregulating the expression of TNF-α. Penitrem E can be used for research on breast cancer.
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- CAS. Nr.: 78213-66-8
- Formel: C37H45NO6
- Molecular Weight:599.76
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
IC50 & Target
[3]|
TNF-α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
17.5 μM
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Antiproliferative activity against human MCF-7 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human MCF-7 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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24273638 |
| MDA-MB-231 | IC50 |
25.4 μM
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Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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24273638 |
| MDA-MB-231 | IC50 |
20.3 μM
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Antimigratory activity against human MDA-MB-231 breast cancer cells assessed as inhibition of cell migration incubated for 24 hrs by wound-healing assay.
Antimigratory activity against human MDA-MB-231 breast cancer cells assessed as inhibition of cell migration incubated for 24 hrs by wound-healing assay.
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24273638 |
| MCF-12A | IC50 |
44.0 μM
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Inhibition of cell growth in non-tumorigenic human MCF-12A mammary epithelial cells incubated for 48 hrs by MTT assay.
Inhibition of cell growth in non-tumorigenic human MCF-12A mammary epithelial cells incubated for 48 hrs by MTT assay.
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29751615 |
| BT-474 | IC50 |
31.8 μM
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Antiproliferative activity against human BT-474 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Antiproliferative activity against human BT-474 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
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29751615 |
| SK-BR-3 | IC50 |
36.7 μM
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Antiproliferative activity against human SK-BR-3 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Antiproliferative activity against human SK-BR-3 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
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29751615 |
In Vitro
Penitrem E (compound 4) exhibits antiproliferative activity against MCF-7 (IC50 17.5 μM) and MDA-MB-231 (IC50 25.4 μM) human breast cancer cells[1].
Penitrem E (compound 4) inhibits migration of MDA-MB-231 cells with an IC50 of 20.3 μM[1].
Penitrem E (compound 4) is inactive in the Cultrex® BME cell invasion assay against MDA-MB-231 cells at 15.0 μM[1].
Penitrem E (48 h) exhibits antiproliferative activity against MDA-MB-231, BT-474, and SK-BR-3 breast cancer cell lines, as well as non-tumorigenic MCF-12A and CRL-2765 cells, with IC50 values ranging from 20.3 to 67.8 µM[2].
Penitrem E (24 h) does not alter KCNMA1 levels but increases TNF-α levels in BT-474 and SK-BR-3 breast cancer cells[2].
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:MDA-MB-231
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Concentration:7.5, 15 μM
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Incubation Time:24 h
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Result:Was inactive at 15.0 μM.
Chemical Information
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CAS. Nr. 78213-66-8
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Molecular Weight 599.76
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Formel C37H45NO6
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SMILES
C=C1CC2=CC=C3C4=C2[C@@]5(O)[C@]1([H])C[C@]5([H])C(C)(C)O[C@@H]([C@@]6([H])[C@@]7(C)[C@](CC[C@@]8([H])[C@]9%10[C@H](O%10)[C@@H](O)[C@@H](C(C)=C)O8)(C)[C@@]9(O)CC6)C4=C7N3
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Structure Classification
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Initial Source
Penicillium crustosum
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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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.
Reinheit & Dokumentation
Verweise
[1]. Sallam AA, et al. Bioguided discovery and pharmacophore modeling of the mycotoxic indole diterpene alkaloids penitrems as breast cancer proliferation, migration, and invasion inhibitors. MedChemComm. 2013 Oct;4(10). [Content Brief]
[2]. Goda AA, et al. The Maxi-K (BK) Channel Antagonist Penitrem A as a Novel Breast Cancer-Targeted Therapeutic. Mar Drugs. 2018 May 11;16(5):157. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Penitrem E Related Classifications
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