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

Related Products

PDF 1.1 MB

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-101791R
    P-gp inhibitor 1 (Standard)
    		Inhibitor
    P-gp inhibitor 1 (Standard) is the analytical standard of P-gp inhibitor 1 (HY-101791). This product is intended for research and analytical applications. P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
    P-gp inhibitor 1 (Standard)
  • HY-13646B
    Encequidar hydrochloride
    		Inhibitor
    Encequidar hydrochloride (HM30181 hydrochloride) is an oral P-glycoprotein (P-gp) inhibitor with the activity of enhancing the oral bioavailability of P-gp substrate drugs. Encequidar shows the highest potency among various MDR1 inhibitors, with IC50=0.63nM. Encequidar effectively blocks the transepithelial transport of paclitaxel in MDCK monolayer cells, with IC50=35.4nM.
    Encequidar hydrochloride
  • HY-N11697
    α-Cryptoxanthin
    		Inhibitor
    α-Cryptoxanthin is a natural carotenoid with anticancer effects. α-Cryptoxanthin inhibits multidrug resistance 1 (MDR1) mediated efflux pump.
    α-Cryptoxanthin
  • HY-N5166
    Ardeemin
    		Inhibitor
    Ardeemin ((-)-Ardeemin) binds to the P-glycoprotein, preventing anticancer agent from being pumped out of cells. Ardeemin reverses the multidrug resistance phenotype of tumor cells and increases the sensitivity of tumor cells to anticancer agent in mammary carcinoma xenografts.
    Ardeemin
  • HY-W035709R
    Hydrocinchonine (Standard)
    		Inhibitor
    Hydrocinchonine (Dihydrocinchonine) (Standard) is the analytical standard of Hydrocinchonine (HY-W035709). This product is used for research and analytical purposes.Hydrocinchonine 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 (Standard)
  • HY-17013AR
    Dofequidar fumarate (Standard)
    		Inhibitor
    Dofequidar (fumarate) (Standard) is the analytical standard of Dofequidar (fumarate). This product is intended for research and analytical applications. Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect.
    Dofequidar fumarate (Standard)
  • HY-108347R
    CP-100356 hydrochloride (Standard)
    		Inhibitor
    CP-100356 hydrochloride (Standard) is the analytical standard of CP-100356 (hydrochloride) (HY-108347). This product is intended for research and analytical applications. CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM).
    CP-100356 hydrochloride (Standard)
  • HY-181114
    P-gp-IN-34
    		Inhibitor
    P-gp-IN-34 (compound 4a) is an Mdr1p (Mdr1 pump) inhibitor. P-gp-IN-34 inhibits yeast to hyphal shift in Candida albicans. P-gp-IN-34 can be used for the research of candidiasis.
    P-gp-IN-34
  • HY-181404
    PA36-2
    		Inhibitor
    PA36-2 is an Mdr1 inhibitor and azole resistance reversal agent, with a IC50 of 1.0 μg/mL and a Kd of 4.209 μM against Candida albicans Mdr1. By effectively inhibiting the activity of the Mdr1 efflux pump, PA36-2 prevents the pumping of substrates out of cells, enhances the intracellular accumulation of azole antibiotics, and exerts a synergistic effect with antifungal agents such as Fluconazole (FLC) (HY-B0101). PA36-2 can be used in the research of azole-resistant candidiasis.
    PA36-2
  • HY-W699430
    Norverapamil-d6 hydrochloride
    		Inhibitor
    Norverapamil-d6 ((±)-Norverapamil-d6) hydrochloride is deuterium labeled Norverapamil (hydrochloride). 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.
    Norverapamil-d<sub>6</sub> hydrochloride
  • HY-16773
    Vedroprevir
    		Inhibitor
    Vedroprevir (GS-9451) is an inhibitor for HCV NS3/4A protease with an IC50 of 3.2 nM. Vedroprevir is also an inhibitor for breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM. Vedroprevir inhibits P-gp, MRP1 and MRP2 with IC50 of 34, 14.9 and 12 μM, respectively. Vedroprevir exhibits good pharmacokinetic characteristics in rats and dogs.
    Vedroprevir
  • HY-50880R
    Elacridar hydrochloride (Standard)
    		Inhibitor
    Elacridar (hydrochloride) (Standard) is the analytical standard of Elacridar (hydrochloride). This product is intended for research and analytical applications. Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer.
    Elacridar hydrochloride (Standard)
  • HY-13646AR
    Encequidar mesylate (Standard)
    		Inhibitor
    Encequidar (mesylate) (Standard) is the analytical standard of Encequidar (mesylate). This product is intended for research and analytical applications. Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
    Encequidar mesylate (Standard)
  • HY-N7305
    Jatrophane 5
    		Inhibitor
    Jatrophane 5 is a natural product of Jatropha carcas L. Jatrophane 5 has powerful inhibition of P-gp, higher than R(+)-verapamil (HY-14275) and Tariquidar (HY-10550) in colorectal multi-drug resistant cells (DLD1-TxR).
    Jatrophane 5
  • HY-164683
    MRP1-IN-1
    		Inhibitor
    MRP1-IN-1 (Compound 9h) is a MRP1 inhibitor with an EC50 of 0.90 μM in HeLa-T5 cells.
    MRP1-IN-1
  • HY-10550AR
    Tariquidar methanesulfonate, hydrate (Standard)
    		Inhibitor
    Tariquidar (methanesulfonate, hydrate) (Standard) is the analytical standard of Tariquidar (methanesulfonate, hydrate). This product is intended for research and analytical applications. Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.
    Tariquidar methanesulfonate, hydrate (Standard)
  • HY-135328
    Norverapamil
    		Inhibitor
    Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
    Norverapamil
  • HY-129698
    MS-073
    		Inhibitor
    MS-073 (CP162398) is a P-glycoprotein (P-gp) inhibitor. MS-073 reverses multidrug resistance in drug-resistant cells by competitively inhibiting drug binding to P-glycoprotein.
    MS-073
Cat. No. Product Name / Synonyms Application Reactivity