P-gp-IN-36
P-gp-IN-36 is a potent P-glycoprotein (P-gp) inhibitor with an EC50 of approximately 1 μM. P-gp-IN-36 inhibits the efflux function of P-glycoprotein, overcoming P-gp-mediated multidrug resistance in cancer cells. P-gp-IN-36 inhibits STAT3 phosphorylation and reduces total STAT3 expression. P-gp-IN-36 sensitizes P-gp-expressing cancer cells to the cytostatic effects of conventional cytostatic drugs. P-gp-IN-36 can be used for the research of multidrug-resistant cancer.
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- Formel: C44H58N4O7
- Molecular Weight:754.95
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Speicherung:
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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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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STAT3 |
P-gp-IN-36 (LD) (0.25-64 μM; 30 min) potently inhibits P-gp in P388/MDR cells, with an EC50 of ~1 μM[1].
P-gp-IN-36 (0.25-64 μM; 30 min) potently inhibits P-gp in CT26 cells[1].
P-gp-IN-36 (15 h) potently inhibits STAT3 signaling in CT26 cells by reducing both STAT3 phosphorylation and total STAT3 protein expression[1].
P-gp-IN-36 (0.5-2 μM; 72 h) potently sensitizes P388/MDR cells to the cytostatic effect of Doxorubicin (HY-15142A), reducing the Doxorubicin IC50 by ~86-fold at a concentration of 2 μM[1].
P-gp-IN-36 (1-4 μM; 48 h) significantly potentiates Doxorubicin-induced apoptosis in P388/MDR cells, reducing live cell populations in a concentration-dependent manner[1].
P-gp-IN-36 (2 μM; 48 h) potentiates Doxorubicin-induced apoptosis in P388/MDR cells by significantly increasing caspase-3 activity at a concentration of 2 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:P388/MDR mouse monocytic leukemia cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:72 h
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Result:Reduced the IC50 of DOX from 8.62 μM (without LD) to 2.29 μM (with 0.5 μM LD), 0.36 μM (with 1 μM LD), and 0.10 μM (with 2 μM LD).
Corresponding to an ~86-fold reduction in DOX IC50 at the highest tested LD concentration.
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Cell Line:P388/MDR mouse monocytic leukemia cells
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Concentration:1, 2, 4 μM
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Incubation Time:48 h
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Result:Decreased the percentage of live cells from 85% (DOX alone) to 68% (DOX + 1 μM LD).
Induced nearly complete apoptosis at 4 μM LD, with the live cell fraction further reduced.
Chemical Information
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Molecular Weight 754.95
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Formel C44H58N4O7
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SMILES
CC(C)[C@H](N1C(NCCC1)=O)C(N[C@@H](CC2=CC=CC=C2)C[C@H](OC(CCC(C(C)C)=O)=O)[C@H](CC3=CC=CC=C3)NC(COC4=C(C)C=CC=C4C)=O)=O
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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
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
P-gp-IN-36 Related Classifications
HY-181773 Related Classifications
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