Crispene E
Crispene E is a STAT3 inhibitor with an IC50 of 10.27 μM against STAT3 dimerization. Crispene E exerts specific cytotoxicity against STAT3-dependent MDA-MB-231 breast cancer cells. Crispene E is applicable to research related to breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 1666128-87-5
- Formula: C20H26O5
- Molecular Weight:346.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
STAT3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
5.35 μM
Compound: 66
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Antiproliferative activity against human MDA-MB-231 cells
Antiproliferative activity against human MDA-MB-231 cells
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[PMID: 34170703] |
In Vitro
Crispene E (0-100 μM; 24 h) selectively reduces the viability of STAT3-dependent MDA-MB-231 breast cancer cells, with an IC50 of 5.35 μM at 24 h, whereas it exhibits much lower activity against STAT3-deficient A4 cells[1].
Crispene E (100 μM; 24 h) downregulates the mRNA expression of STAT3 and its target genes bcl-2, cyclin D1 and fascin in STAT3-dependent MDA-MB-231 breast cancer cells[1].
Crispene E (5 μM; 24 h) selectively downregulates the protein levels of pSTAT3 and fascin in serum-starved, IL-6-treated MDA-MB-231 breast cancer cells, with no effect on pSTAT1[1].
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:STAT3-dependent MDA-MB-231 breast cancer cells
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Concentration:100 μM
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Incubation Time:24 h
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Result:Notably downregulated mRNA expression of STAT3.
Notably downregulated mRNA expression of STAT3-dependent target genes including bcl-2, cyclin D1, and fascin.
Caused particularly significant down-regulation of bcl-2.
Chemical Information
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CAS No. 1666128-87-5
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Molecular Weight 346.42
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Formula C20H26O5
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SMILES
C[C@]12[C@@]34[C@](CC[C@@]1([H])[C@@](C)([C@H](C[C@@]2([H])OC4=O)C)CCC5=CCOC5=O)([H])O3
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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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.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Crispene E Related Classifications
HY-N17494 Related Classifications
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