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-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-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-137433A
    Befotertinib mesylate
    		Inhibitor
    Befotertinib (D-0316) mesylate is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFRT790M, EGFRL858R and delE746-A750, forms covalent bonds with EGFRC797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib mesylate can be used in research related to multidrug-resistant cancers and non-small cell lung cancer.
    Befotertinib mesylate
  • 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
  • HY-17367S3
    Atazanavir-d5
    		Modulator
    Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM.
    Atazanavir-d<sub>5</sub>
  • HY-17367S2
    Atazanavir-d9
    		Modulator
    Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM.
    Atazanavir-d<sub>9</sub>
  • HY-P4902
    Retrocyclin-1
    Retrocyclin-1 is a kind of Theta-defensin. Retrocyclin-1 recognizes and binds to carbohydrate-containing surface molecules, to protect cells from HIV-1 infection. Retrocyclin-1 exhibits high affinity to fetuin, gp120 (Kd=35.4 nM), CD4 (Kd=31 nM), and galactosylceramide (Kd=24.1 nM).
    Retrocyclin-1
  • HY-N4108R
    Hypophyllanthin (Standard)
    		Inhibitor
    Hypophyllanthin (Standard) is the analytical standard of Hypophyllanthin. This product is intended for research and analytical applications. Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity.
    Hypophyllanthin (Standard)
  • HY-135336BS
    (Rac)-Verapamil-d7 (hydrochloride)
    (Rac)-Verapamil-d7 (hydrochloride) is the deuterium labeled (Rac)-Verapamil.
    (Rac)-Verapamil-d<sub>7</sub> (hydrochloride)
  • HY-168711
    P-gp inhibitor 27
    		Inhibitor
    P-gp inhibitor 27 (Compound D2) is an inhibitor for P-glycoprotein (P-gp), that downregulates the expression of P-gp and MRP1, increases the Rh123 accumulation in A2780/T cell, and reverses multidrug resistance to Paclitaxel (HY-B0015) (EC50 is 88 nM) and Cisplatin (HY-17394).
    P-gp inhibitor 27
  • HY-162714
    C3N-Dbn-Trp2
    		Inhibitor
    C3N-Dbn-Trp2 is an inhibitor for ATP-binding cassette transporter ABCB1. C3N-Dbn-Trp2 inhibits the ABCB1-mediated Rhodamine 123 (HY-D0816) efflux in cells HEK293T and HCT-15 with IC50 of 5.9 µM and 2.2 µM. C3N-Dbn-Trp2 inhibits the Doxorubicin (HY-15142A) efflux, enhances the cytotoxicity of Doxorubicin in ABCB1-expressing cells.
    C3N-Dbn-Trp2
Cat. No. Product Name / Synonyms Application Reactivity