2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
  4. P-glycoprotein

P-glycoprotein

P-gp; Pgp; Multidrug resistance protein 1; MDR1; ATP-binding cassette sub-family B member 1; ABCB1; Cluster of differentiation 243; CD243

P-glycoprotein

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P-glycoprotein (P-gp) also known as multidrug resistance protein 1 (MDR1) is an important protein of the cell membrane that pumps many foreign substances out of cells. More formally, it is an ATP-dependent efflux pump with broad substrate specificity. P-gp is extensively distributed and expressed in the intestinal epithelium where it pumps xenobiotics (such as toxins or drugs) back into the intestinal lumen, in liver cells where it pumps them into bile ducts, in the cells of the proximal tubular of the kidney where it pumps them into urine-conducting ducts, and in the capillary endothelial cells comprising the blood–brain barrier and blood-testis barrier, where it pumps them back into the capillaries. Some cancer cells also express large amounts of P-gp, which renders these cancers multi-drug resistant. P-gp is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs. This protein also functions as a transporter in the blood–brain barrier.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-136217
    PU 23
    		Inhibitor 99.48%
    PU 23 is a non-carboxylic multidrug resistance protein 4 (MRP4) inhibitor as an active agent reducing resistance to anticancer agent 6-Mercaptopurine.
    PU 23
  • HY-W035709
    Hydrocinchonine
    		Inhibitor 98.33%
    Hydrocinchonine (Dihydrocinchonine) is a multidrug resistance (MDR)-reversal agent. Hydrocinchonine directly inhibits the function and expression of P-gp, which is the mechanism by which it reverses MDR. Hydrocinchonine exerts synergistic apoptotic effect with Paclitaxel (HY-B0015) in MES-SA/DX5 cells. Hydrocinchonine can be used for the study of gynecological malignant tumors (such as uterine sarcoma) with drug resistance caused by excessive expression of P-gp.
    Hydrocinchonine
  • HY-168528
    WS-917
    		Modulator
    WS-917 is a potent and orally active ABCB1 modulator. WS-917 enhances ABCB1 ATPase activity. WS-917 significantly enhances the antitumor effect of paclitaxel combined with anti-PD-1 antibody. WS-917 promotes CD8+ T-cell activation.
    WS-917
  • HY-N7641
    3',4',7-Trimethoxyquercetin
    		Inhibitor 98.87%
    3',4',7-Trimethoxyquercetin (Quercetin 3′,4′,7-trimethyl ether) is a polymethoxyflavonoid that can be isolated from Taraxacum mongolicum. 3',4',7-Trimethoxyquercetin is also a derivative of Quercetin hydrate (HY-18085A). 3',4',7-Trimethoxyquercetin has anti-tumor activity.
    3',4',7-Trimethoxyquercetin
  • HY-11018A
    Risperidone hydrochloride
    		Inhibitor
    Risperidone hydrochloride (R 64 766 hydrochloride) 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
    Risperidone hydrochloride
  • HY-50879R
    Elacridar (Standard)
    		Inhibitor
    Elacridar (Standard) is the analytical standard of Elacridar. This product is intended for research and analytical applications. Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer.
    Elacridar (Standard)
  • HY-14895
    Fabomotizole
    		Substrate 99.96%
    Fabomotizole (CM346) is an insecticide with anxiolytic, antianxiety, and neuroprotective activities and a substrate of p-glycoprotein. Fabomotizole inhibits the ST-segment depression induced by isoproterenol in a rat model of acute subendocardial ischemia. Fabomotizole also inhibits Giardia lamblia and has the potential to inhibit giardiasis. Fabomotizole also targets Sigma1R, NRH:quinone reductase 2 (NQO2), and MAO-A to exert anxiolytic effects.
    Fabomotizole
  • HY-162373
    α-Amylase/α-Glucosidase-IN-10
    α-Amylase/α-Glucosidase-IN-10 (compound 5d) is an α-amylase and α-glucosidase inhibitor (IC50: 30.39 μM and 65.1 μM) with potential diabetes inhibitory effects. α-Amylase/α-Glucosidase-IN-10 exhibits high gastrointestinal (GI) absorption in ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) prediction. While α-Amylase/α-Glucosidase-IN-10 acts as a substrate for P-gp and does not cross the blood-brain barrier (BBB), there may be a risk of central nervous system side effects.
    α-Amylase/α-Glucosidase-IN-10
  • HY-17411R
    Limonin (Standard)
    		Inhibitor
    Limonin (Standard) is the analytical standard of Limonin. This product is intended for research and analytical applications. Limonin inhibits HIV-1 with an EC50 of 60.0 μM. Limonin induces human colon adenocarcinoma cells apoptosis with an IC50 of 54.74 μM. Limonin has antiviral and antitumor activities.
    Limonin (Standard)
  • HY-11018S2
    Risperidone-d6
    		Inhibitor
    Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
    Risperidone-d<sub>6</sub>
  • HY-110377
    Tariquidar dihydrochloride
    		Inhibitor
    Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).
    Tariquidar dihydrochloride
  • HY-112912
    P-gp modulator 1
    P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
    P-gp modulator 1
  • HY-128685
    FD 12-9
    		Inhibitor
    FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity.
    FD 12-9
  • HY-149053
    OY-101
    		Inhibitor
    OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764).
    OY-101
  • HY-146096
    RMS3
    		Inhibitor
    RMS3, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS3 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS3 has strong anticancer property.
    RMS3
  • HY-170569
    Cetagliptin
    		Substrate
    Cetagliptin is an orally active inhibitor for dipeptidyl peptidase 4 (DPP-4) and CYP2D6 (IC50 of 6 µM). Cetagliptin is a substrate for P-glycoprotein. Cetagliptin reduces the GLP-1 degradation, maintains the level of postprandial blood sugar, and can be used in type 2 diabetes mellitus research.
    Cetagliptin
  • HY-146097
    RMS5
    		Inhibitor
    RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property.
    RMS5
  • HY-10550B
    Tariquidar dimesylate
    		Inhibitor
    Tariquidar dimesylate (XR9576 dimesylate) is a P-glycoprotein (P-gp) inhibitor. Tariquidar dimesylate increases the concentration of the drug in the brain by binding to P-glycoprotein, preventing it from transporting the drug from inside to outside the brain. Tariquidar dimesylate can be used in the study of blood-brain barrier penetration and multidrug resistance.
    Tariquidar dimesylate
  • HY-13646C
    Encequidar mesylate hydrochloride
    		Inhibitor
    Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models.
    Encequidar mesylate hydrochloride
  • HY-B0532B
    Trifluoperazine dimaleate
    		Inhibitor
    Trifluoperazine dimaleate, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dimaleate is a potent α1-adrenergic receptor antagonist. Trifluoperazine dimaleate is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dimaleate is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dimaleate can be used for the research of schizophrenia. Trifluoperazine dimaleate acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine dimaleate
Cat. No. Product Name / Synonyms Application Reactivity