Clausine E
Clausine E, is a alkaloid which can be isolated from Clausena excavata, is a inhibitor of fat mass and obesity-associated protein (FTO) demethylase. Clausine E shows inhibitory activities against proliferation of synoviocytes and cancer cells.
For research use only. We do not sell to patients.
- CAS No.: 182261-83-2
- Formula: C14H11NO3
- Molecular Weight:241.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CNE-2 | IC50 |
16.9 μM
Compound: 3
|
Growth inhibition human CNE2 cells after 48 hrs by WST-8 based CCK8 assay
Growth inhibition human CNE2 cells after 48 hrs by WST-8 based CCK8 assay
|
[PMID: 22093759] |
| HCT-116 | IC50 |
1.9 μM
Compound: clausine E
|
Antiproliferative activity against human HCT116 cells after 72 hrs
Antiproliferative activity against human HCT116 cells after 72 hrs
|
[PMID: 17548198] |
| HeLa | IC50 |
13.3 μM
Compound: 3
|
Growth inhibition human HeLa cells after 48 hrs by WST-8 based CCK8 assay
Growth inhibition human HeLa cells after 48 hrs by WST-8 based CCK8 assay
|
[PMID: 22093759] |
| HepG2 | IC50 |
15.8 μM
Compound: 3
|
Growth inhibition of human HepG2 cells after 48 hrs by WST-8 based CCK8 assay
Growth inhibition of human HepG2 cells after 48 hrs by WST-8 based CCK8 assay
|
[PMID: 22093759] |
| KB | IC50 |
107.56 μM
Compound: 9
|
Cytotoxicity against human KB cells by resazurin microplate assay
Cytotoxicity against human KB cells by resazurin microplate assay
|
[PMID: 21302964] |
| L02 | IC50 |
>160 μM
Compound: 3
|
Cytotoxicity human L02 cells after 48 hrs by WST-8 based CCK8 assay
Cytotoxicity human L02 cells after 48 hrs by WST-8 based CCK8 assay
|
[PMID: 22093759] |
| MCF7 | IC50 |
0.6 μM
Compound: clausine E
|
Antiproliferative activity against human MCF7 cells after 72 hrs
Antiproliferative activity against human MCF7 cells after 72 hrs
|
[PMID: 17548198] |
| MDA-MB-231 | IC50 |
37.1 μM
Compound: 3
|
Growth inhibition human MDA-MB-231 cells after 48 hrs by WST-8 based CCK8 assay
Growth inhibition human MDA-MB-231 cells after 48 hrs by WST-8 based CCK8 assay
|
[PMID: 22093759] |
| MES-SA | IC50 |
35 μM
Compound: clausine E
|
Antiproliferative activity against human Mes-sa cells after 72 hrs
Antiproliferative activity against human Mes-sa cells after 72 hrs
|
[PMID: 17548198] |
| NCI-H187 | IC50 |
94.59 μM
Compound: 9
|
Cytotoxicity against human NCI-H187 by resazurin microplate assay
Cytotoxicity against human NCI-H187 by resazurin microplate assay
|
[PMID: 21302964] |
| SW48 | IC50 |
21 μM
Compound: clausine E
|
Antiproliferative activity against human SW48 cells after 72 hrs
Antiproliferative activity against human SW48 cells after 72 hrs
|
[PMID: 17548198] |
| SW480 | IC50 |
4.8 μM
Compound: clausine E
|
Antiproliferative activity against human SW480 cells after 72 hrs
Antiproliferative activity against human SW480 cells after 72 hrs
|
[PMID: 17548198] |
| T98G | IC50 |
71.6 μM
Compound: 3
|
Growth inhibition human T98G cells after 48 hrs by WST-8 based CCK8 assay
Growth inhibition human T98G cells after 48 hrs by WST-8 based CCK8 assay
|
[PMID: 22093759] |
| Vero | IC50 |
152.05 μM
Compound: 9
|
Cytotoxicity against african green monkey Vero cells by green fluorescent protein microplate assay
Cytotoxicity against african green monkey Vero cells by green fluorescent protein microplate assay
|
[PMID: 21302964] |
Chemical Information
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CAS No. 182261-83-2
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Molecular Weight 241.24
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Formula C14H11NO3
-
SMILES
O=C(C1=CC2=C(NC3=C2C=CC=C3)C(O)=C1)OC
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Synonyms
Clauszoline I
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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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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
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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
[1]. Wang Y, Li J, Han X, et al. Identification of Clausine E as an inhibitor of fat mass and obesity-associated protein (FTO) demethylase activity. J Mol Recognit. 2019;32(10):e2800. [Content Brief]
[2]. Guo JM, Yu XM, Jiang B, et al. Zhongguo Zhong Yao Za Zhi. 2021;46(17):4438-4445. [Content Brief]
[3]. Liger F, Popowycz F, Besson T, Picot L, Galmarini CM, Joseph B. Synthesis and antiproliferative activity of clausine E, mukonine, and koenoline bioisosteres. Bioorg Med Chem. 2007;15(16):5615-5619. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)