Lobetyol
Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity. Lobetyol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- No. CAS: 136171-87-4
- Fòrmula: C14H18O3
- Peso molecular:234.29
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Actividad biológica
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Bax |
Bcl-2 |
Lobetyol (0-100 μg/mL, 0-48 h) leads to a dose-and time-dependent proliferation inhibition in MKN45 cells[1].
Lobetyol (0-100 μg/mL, 48 h) induces apoptosis and cell cycle arrest in a time- and dose-dependent manner in MKN45 cells[1].
Lobetyol (0-100 μg/mL, 48 h) increases the expression level of Bax, P53, and decreased the expression level of Bcl-2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MKN45 cells
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Concentration:0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL
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Incubation Time:12 h, 24 h, 48 h
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Result:Showed a dose-and time-dependent proliferation inhibition in MKN45 cells, with an IC50 of 71.47 ± 4.29 μg/mL at 48 h. Exhibited more safety on L02 and HEK293 human normal cell lines.
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Cell Line:MKN45 cells
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Concentration:0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL
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Incubation Time:48 h
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Result:Increased the apoptotic population in MKN45 cells in a dose-dependent manner. Flow cytometic assay of Annexin-V/PI revealed apoptotic populations under increasing dose of lobetyol ranging from 0 μg/mL, 50 μg/mL, 75 μg/mL, to 100 μg/mL are 5.5%, 13.74%, 27.32% to 31.57%, respectively.
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Cell Line:MKN45 cells
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Concentration:0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL
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Incubation Time:12 h, 24 h, 48 h
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Result:Increased the expression level of Bax, P53, and decreased the expression level of Bcl-2. The release of cytochrome c was detected, followed by caspase-9 and -3 activations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C nude mice (6 weeks-old, injected intraperitoneally with MKN45 cells)[1]
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Dosage:0, 2, 5, 10 mg/kg
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Administration:Once per 3 days
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Result:Suppressed tumor growth in MKN45 nude models. The protein levels of Ki67 in MKN45 cells were significantly decreased. Meanwhile, cleaved-caspase-3 positive MKN45 cells were found increased with the tendency of lobetyol concentrations in the study in vivo.
Chemical Information
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No. CAS 136171-87-4
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Peso molecular 234.29
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Fòrmula C14H18O3
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SMILES
C/C=C/C#CC#CC(O)C(O)/C=C/CCCO
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Structure Classification
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Initial Source
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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]. Shen J, et al. Lobetyol activate MAPK pathways associated with G1/S cell cycle arrest and apoptosis in MKN45 cells in vitro and in vivo. Biomed Pharmacother. 2016 Jul;81:120-127. [Content Brief]
[2]. Xie Q, et al. The in vitro/in vivo metabolic pathways analysis of lobetyol, lobetyolin, and lobetyolinin, three polyacetylenes from Codonopsis Radix, by UHPLC-Q/TOF-MS and UHPLC-MS/MS. J Pharm Biomed Anal. 2023 Jan 20;223:115140. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lobetyol Related Classifications
HY-117652 Related Classifications
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