Limocitrin
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Limocitrin is a flavonol glycoside. Limocitrin inhibits AKT phosphorylation and JNK phosphorylation, upregulates p38 phosphorylation, and inhibits ERK1/2 phosphorylation, thereby blocking MAPK signaling. Limocitrin induces Apoptosis through the mitochondrial pathway, death receptor-mediated signaling, Caspase activation, and G2/M cell cycle arrest. Limocitrin possesses anti-inflammatory and anticancer properties. Limocitrin can be used for research on oral squamous cell carcinoma and chronic myeloid leukemia.
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- Pureté : 99.58%
- CAS No.: 489-33-8
- Formule: C17H14O8
- Masse moléculaire:346.29
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Stockage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
Description
IC50 & Target
[1]|
ERK1 |
ERK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Monocyte | IC50 |
67 μM
Compound: Limocitrin
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Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA
Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA
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[PMID: 10096854] |
In Vitro
Limocitrin (0-40 µM; 24 h) exerts a strong antiproliferative effect on SCC-9 and SCC-47 oral cancer cells by reducing colony formation[1].
Limocitrin (5-20 μM; 72 h) enhances the cytotoxicity of KHYG-1 cells against K562 cells[2].
Limocitrin (0-40 µM; 24 h) induces apoptosis in SCC-9 and SCC-47 oral cancer cells by modulating the expression of Bcl-2 family proteins and death receptor-related proteins[1].
Limocitrin (5-20 μM; 24 h) increases the protein expression of cytolytic effector molecules perforin, granzyme A and B, and granulysin in KHYG-1 cells[2].
Limocitrin (5-20 μM; 24 h) dose-dependently increases CREB phosphorylation and histone H3 acetylation in KHYG-1 cells[2].
Limocitrin (5-20 μM; 24 h) dose-dependently increases mitochondrial membrane depolarization in K562 cells co-cultured with KHYG-1 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SCC-9 and SCC-47
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Concentration:0, 10, 20, 40 µM
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Incubation Time:24, 48, and 72 h
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Result:Inhibited the viability of SCC-9 and SCC-47 cells in a concentration-dependent and time-dependent manner.
Found the effective dose to inhibit SCC-9 to be 40 µM at 48 h and 72 h treatment.
Inhibited only 40% of SCC-47 cell viability at 40 µM until 72 h treatment.
Showed a better cell inhibitory effect on SCC-9 cells than SCC-47 cells.
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Cell Line:SCC-47 and SCC-9
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Concentration:0, 10, 20, 40 µM
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Incubation Time:24 h
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Result:Dramatically reduced the number of colonies in SCC-9 and SCC-47 oral cancer cells in a concentration-dependent manner.
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Cell Line:SCC-9 and SCC-47
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Concentration:0, 10, 20, 40 µM
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Incubation Time:24 h
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Result:Increased the expression of pro-apoptotic proteins Bax and Bak and decreased the expression of anti-apoptotic proteins Bcl-xL and Bcl-2.
Increased the expression of Fas, DcR2, DcR3, and DR5 compared with the control group.
Slightly increased Fas and DR5 expression in both cancer cell lines.
Greatly increased DcR3 in SCC-9 cells.
Significantly increased DcR2 expression more than DcR3 expression in SCC-47 cells.\nDecreased Cyclin E1 and E2 expression and increased p21 expression in a dose-dependent manner.
Potently downregulated CDK2, CDK4, and CDK6 expression levels.\nResulted in dose-dependent inhibition of XIAP, cIAP-1, and pHSP-27 protein expression in SCC-9 and SCC-47 cells.
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Cell Line:SCC-9 and SCC-47
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Concentration:0, 10, 20, 40 µM
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Incubation Time:24 h
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Result:Significantly enhanced the apoptosis rates of SCC-9 and SCC-47 cells.
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Cell Line:KHYG-1
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Concentration:5-20 μM
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Incubation Time:24 h
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Result:Significantly increased the protein expressions of perforin, granzymes A and B, and granulysin.\nSignificantly and dose-dependently elevated the expression of phosphorylated CREB.
Significantly increased the expression of acetyl-histone H3.
- Kinase activity and phosphorylation assays
- Western Blot
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Protocol for Kinase activity and phosphorylation assays
- Research Protocol for Inflammation-related Diseases
Chemical Information
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CAS No. 489-33-8
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Appearance Solid
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Masse moléculaire 346.29
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Formule C17H14O8
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Color Light yellow to yellow
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SMILES
O=C1C(O)=C(OC2=C(C(O)=CC(O)=C12)OC)C3=CC(OC)=C(C=C3)O
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Pureté et documentation
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Fiche technique (289 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)