1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. P-gp inhibitor 1

P-gp inhibitor 1 

Cat. No.: HY-101791
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P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

For research use only. We do not sell to patients.

P-gp inhibitor 1 Chemical Structure

P-gp inhibitor 1 Chemical Structure

CAS No. : 2050747-49-2

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Description

P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

IC50 & Target

P-glycoprotein[1]

In Vitro

P-gp inhibitor 1 (12k) possesses high potency (EC50=57.9±3.5 nM), low cytotoxicity, and long duration of activity in reversing doxorubicin (DOX) resistance in K562/A02 cells (1 μM, 80 minutes)[1].

P-gp inhibitor 1 also boosts the potency of other MDR-related cytotoxic agents with different structures, increases accumulation of DOX, blocks Pgp-mediated Rh123 efflux, and suppresses P-gp ATPase activity in K562/A02 MDR cells (0.1, 1, 5 μM, 1 hour)[1].

Western Blot Analysis[1]

Cell Line: K562/A02 cell
Concentration: 0.1, 0.5, or 2.0 μM
Incubation Time: 72 hours
Result: MDR reversal by 12k was not caused by a decreased protein expression but instead most likely due to direct inhibition of P-gp efflux[1].
Molecular Weight

517.62

Formula

C₃₂H₃₁N₅O₂

CAS No.

2050747-49-2

SMILES

COC(C(OC)=C1)=CC2=C1CCN(C2)CCC3=CC=C(NC4=NC(C5=CC=NC=C5)=NC6=CC=CC=C46)C=C3

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

P-gp inhibitor 1P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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P-gp inhibitor 1
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