1. Membrane Transporter/Ion Channel Stem Cell/Wnt JAK/STAT Signaling
  2. P-glycoprotein STAT
  3. 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.

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

P-gp-IN-36

P-gp-IN-36 Chemical Structure

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Description

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[1].

IC50 & Target[1]

STAT3

 

In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: P388/MDR mouse monocytic leukemia cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 72 h
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.

Apoptosis Analysis[1]

Cell Line: P388/MDR mouse monocytic leukemia cells
Concentration: 1, 2, 4 μM
Incubation Time: 48 h
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.
Molecular Weight

754.95

Formula

C44H58N4O7

SMILES

CC1=CC=CC(C)=C1OCC(N[C@@H](CC2=CC=CC=C2)C(C[C@@H](CC3=CC=CC=C3)NC([C@H](C(C)C)N4CCCNC4=O)=O)OC(CCC(C(C)C)=O)=O)=O

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

Purity & Documentation
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  • 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.

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Product Name:
P-gp-IN-36
Cat. No.:
HY-181773
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