Chikusetsusaponin IVa methyl ester
Chikusetsusaponin IVa methyl ester (CME) is a natural triterpenoid saponin compound. Chikusetsusaponin IVa methyl ester induces G0/G1 cell cycle arrest and apoptosis in colon cancer cells by inhibiting the Wnt/β-catenin signaling pathway. By inhibiting the NF-κB and AP-1 signaling pathways, Chikusetsusaponin IVa methyl ester significantly reduces the production of NO, PGE₂ and pro-inflammatory cytokines (TNF-α, IL-6, IL-1β), and downregulates the levels of iNOS and COX-2. Chikusetsusaponin IVa methyl ester can be used in researches on colorectal cancer and inflammation.
For research use only. We do not sell to patients.
- CAS No.: 58546-61-5
- Formula: C43H68O14
- Molecular Weight:808.99
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Neutrophil | IC50 |
1.97 μM
Compound: 7
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Inhibition of fMLP/CB-activated human neutrophil degranulation assessed as inhibition of elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as a substrate after 5 mins
Inhibition of fMLP/CB-activated human neutrophil degranulation assessed as inhibition of elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as a substrate after 5 mins
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[PMID: 21417387] |
Chikusetsusaponin IVa methyl ester (3-30 μM；7-25 h) concentration-dependently inhibits LPS-induced pro-inflammatory mediator production and gene expression in RAW264.7 macrophages via suppression of iNOS, COX-2, TNF-α, IL-6, and IL-1β expression[1].
Chikusetsusaponin IVa methyl ester (3-30 μM; 1 h pretreatment, 15-45 min/18 h LPS treatment) concentration-dependently inhibits LPS-induced NF-κB and AP-1 activation in RAW264.7 macrophages via suppression of NF-κB p65 nuclear translocation and c-Fos expression/phosphorylation[1].
Chikusetsusaponin IVa methyl ester (12.5-100 μM; 24 h) inhibits cell proliferation in HCT116 cells with decreased viability at 25 μM and severe cell death above 50 μM[2].
Chikusetsusaponin IVa methyl ester (10-40 μM) induces G0/G1 cell cycle arrest in HCT116 cells[2].
Chikusetsusaponin IVa methyl ester (20-30 μM; 4-24 h) downregulates cyclin D1, CDK2, and CDK4 and upregulates p21 in HCT116 cells in vitro in a time- and dose-dependent manner[2].
Chikusetsusaponin IVa methyl ester (20-30 μM; 24 h) reduces β-catenin binding to TBE in HCT116 cells in a dose-dependent manner[2].
Chikusetsusaponin IVa methyl ester (20-30 μM; 24 h) reduces nuclear β-catenin levels in HCT116 cells in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7
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Concentration:3 μM, 15 μM, 30 μM
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Incubation Time:Pre-treatment for 1 h, followed by LPS stimulation for 6 h
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Result:Concentration-dependently inhibited the mRNA expression of iNOS, COX-2, TNF-α, IL-6 and IL-1β.
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Cell Line:RAW264.7
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Concentration:3 μM, 15 μM, 30 μM
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Incubation Time:Pre-treatment for 1 h, followed by LPS stimulation for 24 h
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Result:Concentration-dependently inhibited the protein expression of iNOS, COX-2, TNF-α, IL-6 and IL-1β.
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Cell Line:HCT116 colon cancer cells
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Concentration:12.5, 25, 50 and 100 μM
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Incubation Time:24 h
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Result:Decreased cell proliferation at 25 μM and 50 μM; caused severe cell death at concentrations above 50 μM.
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Cell Line:HCT116 colon cancer cells
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Concentration:20, 30 μM
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Incubation Time:4 h, 8 h, 24 h
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Result:Decreased cyclin D1, CDK2, and CDK4 expression in a time- and dose-dependent manner; increased p21 expression.
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Cell Line:HCT116 colon cancer cells
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Concentration:30 μM
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Incubation Time:0 h, 6 h, 24 h
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Result:Suppressed the nuclear translocation of β-catenin over time.
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Cell Line:HCT116 colon cancer cells
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Concentration:20, 30 μM
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Incubation Time:24 h
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Result:Decreased the level of β-catenin in the nucleus in a dose-dependent manner.
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Cell Line:HCT116 colon cancer cells
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Concentration:20, 30 μM
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Incubation Time:24 h
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Result:Decreased the mRNA expression of cyclin D1 and c-myc.
Chemical Information
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CAS No. 58546-61-5
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Molecular Weight 808.99
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Formula C43H68O14
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SMILES
OC[C@H]([C@H]([C@@H]([C@H]1O)O)O)O[C@H]1OC([C@]23[C@](CC(C)(CC3)C)([H])C4=CC[C@@]([C@@]5([C@@](C(C)([C@H](CC5)O[C@@H]6O[C@@H]([C@H]([C@@H]([C@H]6O)O)O)C(OC)=O)C)([H])CC7)C)([H])[C@]7(C)[C@@]4(CC2)C)=O
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Synonyms
CME
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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.
Purity & Documentation
References
[1]. Lee HJ, et al. Chikusetsusaponin IVa Methyl Ester Isolated from the Roots of Achyranthes japonica Suppresses LPS-Induced iNOS, TNF-α, IL-6, and IL-1β Expression by NF-κB and AP-1 Inactivation. Biol Pharm Bull. 2016;39(5):657-664. [Content Brief]
[2]. Lee KM, et al. Chikusetsusaponin IVa methyl ester induces cell cycle arrest by the inhibition of nuclear translocation of β-catenin in HCT116 cells. Biochem Biophys Res Commun. 2015;459(4):591-596. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Chikusetsusaponin IVa methyl ester Related Classifications
HY-N17736 Related Classifications
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- Chikusetsusaponin IVa methyl ester
- 58546-61-5
- CME
- NF-κB
- COX
- Interleukin Related
- TNF Receptor
- NO Synthase
- Prostaglandin Receptor
- CDK
- β-catenin
- Wnt
- Apoptosis
- nitric oxide (NO)
- macrophages
- p65 subunit
- interleukin-6 (IL-6)
- Nuclear factor-kappaB (NF-κB)
- prostaglandin E2 (PGE2)
- tumor necrosis factor-alpha (TNF-α)
- c-Fos
- Activator protein-1 (AP-1)
- Inhibitor
- inhibitor
- inhibit