1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. 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 (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-N4108
    Hypophyllanthin
    Inhibitor 98.84%
    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
  • HY-139848
    WS-898
    Inhibitor 98.51%
    WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively).
    WS-898
  • 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-N0797R
    (20S)-Protopanaxadiol (Standard)
    Inhibitor
    (20S)-Protopanaxadiol (Standard) is the analytical standard of (20S)-Protopanaxadiol. This product is intended for research and analytical applications. 20S-protopanaxadiol (aPPD) is a metabolite of ginseng saponins, inhibits Akt activity and induces apoptosis in various tumor cells.
    (20S)-Protopanaxadiol (Standard)
  • 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-14275R
    Verapamil (Standard)
    Inhibitor
    Verapamil (Standard) is the analytical standard of Verapamil. This product is intended for research and analytical applications. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.
    Verapamil (Standard)
  • 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-19626
    NSC23925
    Inhibitor 99.43%
    NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor.
    NSC23925
  • HY-101791
    P-gp inhibitor 1
    Inhibitor 98.79%
    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
    P-gp inhibitor 1
  • HY-110232
    Risperidone-d4
    Inhibitor 99.34%
    Risperidone-d4 is the deuterium labeled Risperidone. 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>4</sub>
  • HY-119101
    AZD-5672
    Inhibitor
    AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis.
    AZD-5672
  • HY-N3085
    Phellamurin
    Inhibitor
    Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity.
    Phellamurin
  • HY-143792
    HTT-D3
    Inhibitor
    HTT-D3 is an orally active, blood-brain barrier penetrant splicing modulator of huntingtin (HTT). HTT-D3 promotes the inclusion of a pseudo-exon containing a premature termination codon into HTT pre-mRNA, triggers nonsense-mediated mRNA degradation and reduces HTT protein levels. HTT-D3 induces dose-dependent, comparable reductions in mutant HTT protein in both the brain and peripheral tissues of transgenic mouse models. HTT-D3 can be used for the research of Huntington's disease.
    HTT-D3
  • HY-132866
    YS-370
    Inhibitor 98.07%
    YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity.
    YS-370
  • HY-N1423S1
    Glycocholic acid-d5
    Inhibitor 99.9%
    Glycocholic acid-d5 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid-d<sub>5</sub>
  • HY-B0532AR
    Trifluoperazine dihydrochloride (Standard)
    Inhibitor
    Trifluoperazine (dihydrochloride) (Standard) is the analytical standard of Trifluoperazine (dihydrochloride). This product is intended for research and analytical applications. Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine dihydrochloride (Standard)
  • HY-155391
    hCA/Wnt/β-catenin-IN-1
    Inhibitor 99.96%
    hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor of hCA (Ki: 33.6, 24.1, 6.8 nM for hCA II, hCA IX, hCA XII). hCA/Wnt/β-catenin-IN-1 reduces P-gp activity. hCA/Wnt/β-catenin-IN-1 also inhibits Wnt/β-catenin signaling pathway. hCA/Wnt/β-catenin-IN-1 inhibits cancer cell viability, including the NCI/ADR-RES DOX-resistant cell line.
    hCA/Wnt/β-catenin-IN-1
  • HY-N0007AR
    Bisdemethoxycucurmin (Standard)
    Inhibitor
    Bisdemethoxycucurmin (Standard) (Curcumin III (Standard)) is the analytical standard of Bisdemethoxycucurmin (HY-N0007A). This product is intended for research and analytical applications. Bisdemethoxycucurmin (Curcumin III) is a curcuminoid compound and an inhibitor of P-glycoprotein and ferroptosis. Bisdemethoxycucurmin exhibits multiple activities such as anti-oxidation, anti-inflammation and anti-tumor. Bisdemethoxycucurmin can be used for the research of tumors and inflammatory diseases.
    Bisdemethoxycucurmin (Standard)
  • HY-136589
    Verapamil EP Impurity C hydrochloride
    Inhibitor 99.61%
    NSC-609249 hydrochloride is an impurity of Verapamil (HY-14275). Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.
    Verapamil EP Impurity C hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity