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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- No. CAS: 78213-66-8
- Fòrmula: C37H45NO6
- Peso molecular:599.76
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
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.
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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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No. CAS 78213-66-8
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Peso molecular 599.76
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Penitrem E Related Classifications
HY-N22060 Related Classifications
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