P-gp inhibitor 5
P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-InTM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015).
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- CAS. Nr.: 2451298-06-7
- Formel: C28H20ClNO5S
- Molecular Weight:517.98
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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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Biologische Aktivität
Beschreibung
IC50 & Target
P-gp[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Flp-In-293 | IC50 |
>40 μM
Compound: 10
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Cytotoxicity against Flp-In-293 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
Cytotoxicity against Flp-In-293 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
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[PMID: 32569926] |
| Flp-In-293 | IC50 |
29.7 μM
Compound: 10
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Cytotoxicity against Flp-In-293 cells expressing human ABCB1 assessed as reduction in cell viability measured after 72 hrs by SRB assay
Cytotoxicity against Flp-In-293 cells expressing human ABCB1 assessed as reduction in cell viability measured after 72 hrs by SRB assay
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[PMID: 32569926] |
| HeLa | IC50 |
>40 μM
Compound: 10
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
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[PMID: 32569926] |
In Vitro
P-gp inhibitor 5 (compound 10) has cytotoxic against ABCB1/Flp-InTM-293 and KBvin cells with IC50s of 29.7 and 12.6 μM, respectively[1].
P-gp inhibitor 5 (2.5 and 5 μM) lows the IC50s of KBvin cells for Vincristine to 7.59~36.82 nM, for Paclitaxel to 21.0~79.5 nM, for Doxorubicin to 85.7~111 nM; lows the IC50s of HeLaS3 cells for Vincristine to 2.24~3.91 nM, for Paclitaxel to 8.81~9.58 nM, for Doxorubicin to 102~1260 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS. Nr. 2451298-06-7
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Molecular Weight 517.98
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Formel C28H20ClNO5S
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SMILES
O=C(NC1=C(C2=CC=CS2)C3=C(OC(C)=O)C=C(C4=CC=C(OC)C=C4)C=C3O1)C5=CC=CC=C5Cl
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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.
Protokoll
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
P-gp inhibitor 5 Related Classifications
HY-150565 Related Classifications
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