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-149366
    ABCB1-IN-1
    		Inhibitor
    ABCB1-IN-1 (compound 3) is a potent ABCB1 inhibitor. ABCB1-IN-1 induces cell apoptosis. ABCB1-IN-1 bearing 1-benzylimidazole has IC50 values of 1.26 μM and 2.21 μM for Colo205 and Colo320 cells, respectively.
    ABCB1-IN-1
  • 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-N10563
    Coleon-U-quinone
    		Inhibitor
    Coleon-U-quinone is a potent P-gp inhibitor. Coleon-U-quinone can inhibit cancer cells viability and sensitize multidrug resistance cancer cells to Doxorubicin (HY-15142A).
    Coleon-U-quinone
  • HY-146118
    P-gp modulator 3
    		Modulator
    P-gp modulator 3 (Compound 37) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator.
    P-gp modulator 3
  • HY-17367AR
    Atazanavir (sulfate) (Standard)
    		Modulator
    Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM.
    Atazanavir (sulfate) (Standard)
  • HY-14275S1
    Verapamil-d7
    		Inhibitor
    Verapamil-d7 is the deuterium labeled Verapamil (HY-14275). 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-d<sub>7</sub>
  • HY-W230975
    (E/Z)-Piperine
    		Inhibitor 98.91%
    (E/Z)-Piperine ((E/Z)-Bioperine) is an alkaloid with a pungent property. (E/Z)-Piperine shows anti-inflammation, immunomodulatory and anti-cancer, antispasmodic and anti-secretory effects. (E/Z)-Piperine demonstrates significant neuroprotective effect in Alzheimer’s disease and Parkinson’s disease.
    (E/Z)-Piperine
  • HY-121247
    Bromotetrandrine
    		Inhibitor
    Bromotetrandrine is a potent inhibitor of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR). Bromotetrandrine shows significant MDR reversal activity in vitro and in vivo, which may be related to the inhibition of P-gp overexpression and the increase in intracellular accumulation of anticancer agents. Bromotetrandrine is a brominated derivative of tetrandrine, which is promising for MDR modulator for tumor assessment.
    Bromotetrandrine
  • HY-100750R
    Norverapamil hydrochloride (Standard)
    		Inhibitor
    Norverapamil (hydrochloride) (Standard) is the analytical standard of Norverapamil (hydrochloride). This product is intended for research and analytical applications. Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
    Norverapamil hydrochloride (Standard)
  • HY-107212R
    Selamectin (Standard)
    		Inhibitor
    Selamectin (Standard) is the analytical standard of Selamectin. This product is intended for research and analytical applications. Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.
    Selamectin (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
  • HY-W702292
    (R)-(+)-Verapamil-d6 hydrochloride
    		Inhibitor
    (R)-(+)-Verapamil-d6 (hydrochloride) is deuterium labeled (R)-Verapamil (hydrochloride). (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents.
    (R)-(+)-Verapamil-d<sub>6</sub> hydrochloride
  • HY-161353
    c-Met-IN-23
    		Inhibitor
    c-Met-IN-23 (Compound 12g) is a c-Met inhibitor (IC50 = 0.052 μM for c-Met). c-Met-IN-23 also inhibits MDR1 and MRP1/2 pumps in the cancerous HepG2 and BxPC3 cells. c-Met-IN-23 is an anticancer agent.
    c-Met-IN-23
  • HY-129841
    Niguldipine monohydrochloride
    		Inhibitor
    Niguldipine monohydrochloride is a calcium channel blocker that inhibits P-glycoprotein and can be used in tumor research. Niguldipine monohydrochloride inhibits Cav 3.2, with an IC50 of 0.9 μM.
    Niguldipine monohydrochloride
  • HY-162822
    P-gp modulator-5
    		Modulator
    P-gp modulator-5 (compound 25) is a modulator of P-gp and can inhibit the proliferation of multidrug resistant (MDR) tumors. P-gp modulator-5 inhibits the activity of drug efflux pumps in MDR cells, leading to a large accumulation of ROS and altered cell cycle profiles.
    P-gp modulator-5
  • HY-146389
    Anticancer agent 50
    		Modulator
    Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma.
    Anticancer agent 50
  • HY-163981
    ABCB1-IN-2
    		Inhibitor
    ABCB1-IN-2 (compound 16q) is a functional inhibitor that can directly bind to the ABCB1 protein and stabilize its structure without affecting the expression and subcellular localization of ABCB1. ABCB1-IN-2 can increase the sensitivity of MCF-7/ADR cells to paclitaxel (PTX), increase the accumulation of PTX, and prevent the accumulation and excretion of luciferin Rh123 mediated by ABCB1. ABCB1-IN-2, as an ABCB1-mediated multidrug resistance (MDR) reversal agent, shows a strong ability to reverse MDR.
    ABCB1-IN-2
  • HY-155152
    P-gp/BCRP-IN-2
    		Inhibitor
    P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells.
    P-gp/BCRP-IN-2
  • HY-157876
    Anticancer agent 191
    		Inhibitor
    Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research.
    Anticancer agent 191
  • HY-146391
    P-gp inhibitor 4
    		Modulator
    P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases agent transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells.
    P-gp inhibitor 4
Cat. No. Product Name / Synonyms Application Reactivity