2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. 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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P-gp inhibitor 5 Chemical Structure

P-gp inhibitor 5 Chemical Structure

CAS No. : 2451298-06-7

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P-gp inhibitor 5 Related Antibodies

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Description

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)[1].

IC50 & Target

P-gp[1]
Cellular Effect
Cell Line Type Value Description References
Flp-In-293 IC50
> 40 μM
Compound: 10
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
[PMID: 32569926]
Flp-In-293 IC50
29.7 μM
Compound: 10
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
[PMID: 32569926]
HeLa IC50
> 40 μM
Compound: 10
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
[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.

P-gp inhibitor 5 Related Antibodies
Molecular Weight

517.98

Formula

C28H20ClNO5S
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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P-gp inhibitor 5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

P-gp inhibitor 52451298-06-7P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243KBvinVincristinePaclitaxelDoxorubicinmultidrug resistanceantiproliferativeInhibitorinhibitorinhibit

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HY-150565
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