Pyramidatine
Pyramidatine (Haplamidine) is a P-glycoprotein inhibitor with an IC50 of 39.29 µM. As a sensitizer, Pyramidatine enhances Vincristine (HY-N0488A)-induced Apoptosis and G2/M phase arrest, while potentiating the activity of Vincristine against drug-resistant oral cancer. Pyramidatine can be used in research related to oral cancer and mammary adenocarcinoma.
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- CAS. Nr.: 64223-54-7
- Formel: C20H22N2O2
- Molecular Weight:322.41
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Pyramidatine (10 µM; 24 h) enhances VCR-induced apoptosis in KB/VCR cells, increasing the apoptotic rate to 31.31% when used at 10 µM in combination with 0.2 µM VCR for 24 h[1].
Pyramidatine (10 µM; 48 h) upregulates pro-apoptotic marker expression in KB/VCR cells when used at 10 µM in combination with 0.2 µM VCR for 48 h[1].
Pyramidatine (10 µM; 24 h) enhances VCR-induced G2/M arrest in KB/VCR cells, resulting in 97.44% of cells arrested in G2/M phase when used at 10 µM in combination with 0.2 µM VCR for 24 h[1].
Pyramidatine inhibits Verapamil (HY-14275)-stimulated P-gp ATPase activity in recombinant human P-gp membranes with an IC50 of 39.29 µM[1].
Pyramidatine (10 µM; 36 h) suppresses P-gp protein expression in KB/VCR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KB/VCR cells
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Concentration:10 µM (alone); 10 µM (combined with 0.2 µM VCR)
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Incubation Time:24 h
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Result:Induced 6.59% apoptosis in KB/VCR cells when used alone at 10 µM.
Increased the apoptotic rate to 31.31% when combined with 0.2 µM VCR, which was 2.13-fold higher than VCR alone (14.73%) and higher than the verapamil-positive control combination (21.83%).
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Cell Line:KB/VCR cells
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Concentration:10 µM (alone); 10 µM (combined with 0.2 µM VCR)
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Incubation Time:48 h
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Result:Significantly increased the expression of cleaved PARP and pro-apoptotic Bax protein in KB/VCR cells when combined with 0.2 µM VCR.
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Cell Line:KB/VCR cells
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Concentration:10 µM (alone); 10 µM (combined with 0.2 µM VCR)
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Incubation Time:24 h
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Result:Resulted in 22.41% of KB/VCR cells arrested in G2/M phase when used alone at 10 µM.
Increased the G2/M arrest rate to 97.44% when combined with 0.2 µM VCR, which was higher than VCR alone (63.18%) and the verapamil-positive control combination (89.57%).
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Cell Line:KB/VCR cells
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Concentration:10 µM (alone); 10 µM (combined with 0.2 µM VCR)
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Incubation Time:24 h
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Result:Increased cyclin B1 protein expression in KB/VCR cells when combined with 0.2 µM VCR.
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Cell Line:KB/VCR cells
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Concentration:10 µM
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Incubation Time:36 h
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Result:Significantly decreased P-gp protein expression in KB/VCR cells, which naturally overexpress P-gp compared to parental KB cells.
Chemical Information
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CAS. Nr. 64223-54-7
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Molecular Weight 322.41
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Formel C20H22N2O2
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SMILES
C(NCCCCNC(/C=C/C1=CC=CC=C1)=O)(=O)C2=CC=CC=C2
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Synonyms
Haplamidine
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Liu Z, et al. Pyramidatine (Z88) Sensitizes Vincristine-Resistant Human Oral Cancer (KB/VCR) Cells to Chemotherapeutic Agents by Inhibition of P-glycoprotein. Anti-cancer agents in medicinal chemistry. 2018;18(2):286-294. [Content Brief]
[2]. Saifah E, et al. Bisamides from Aglaia species: structure analysis and potential to reverse drug resistance with cultured cells. Journal of natural products. 1993 Apr;56(4):473-7. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Pyramidatine Related Classifications
HY-187041 Related Classifications
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