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-162753
    ZW-1226
    		Inhibitor 98.13%
    ZW-1226 is a selective inhibitor of MRP1, reducing the uptake activity of MRP1 vesicles by 65 % at 5 μM. ZW-1226 shows inhibition of MRP1 in a GSH dependent way and good selectivity for MRP1 over other major ABC transporters, including P-gp, BCRP, MRP2 and MRP3.
    ZW-1226
  • HY-A0064S
    Verapamil-d3 hydrochloride
    		Inhibitor 99.57%
    Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.
    Verapamil-d<sub>3</sub> hydrochloride
  • HY-106004
    Zamicastat
    		Inhibitor 99.93%
    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. Zamicastat reduces high blood pressure.
    Zamicastat
  • HY-N6932
    Voacamine
    		Inhibitor 99.64%
    Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits EGFR to exert oncogenic activity against colorectal cancer.
    Voacamine
  • HY-128878
    Dexloxiglumide
    		98.25%
    Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors.
    Dexloxiglumide
  • HY-17013
    Dofequidar
    		Inhibitor 98.17%
    Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar 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
  • HY-P10856
    CPI1
    		Inhibitor 98.34%
    CPI1 is a potent and highly specific multidrug resistance protein 1 (MRP1) inhibitor. CPI1 inhibits MRP1 (Ki: 100 nM) with nanomolar potency but shows minimal inhibition of P-glycoprotein (Pgp). CPI1 and LTC4 compete to bind to the same site of MRP1, inhibiting ATP hydrolysis and substrate transport. CPI1 can be used to study drug delivery and chemotherapy resistance in cancer.
    CPI1
  • HY-119823
    PGP-4008
    		Inhibitor 99.26%
    PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple agent resistance (MDR) solid tumor model when given in combination with Doxorubicin.
    PGP-4008
  • HY-126940
    Furanodiene
    		Inhibitor 99.83%
    Furanodiene is a natural terpenoid isolated from Rhizoma Curcumae. Furanodiene plays anti-cancer effects through anti-angiogenesis and inducing ROS production, DNA strand breaks and apoptosis. Furanodiene suppresseed efflux transporter Pgp (P-glycoprotein) function and reduced Pgp protein level.
    Furanodiene
  • HY-N6015
    Bacopasaponin C
    		Inhibitor 99.76%
    Bacopasaponin C is an orally active natural glycoside. Bacopasaponin C can be isolated from Bacopa monniera. Bacopasaponin C inhibits Verapamil (HY-14275)-stimulated P-gp ATPase activity with an IC50 of 57.83 μg/mL. Bacopasaponin C has antitumor activity against sarcomas. Bacopasaponin C has antiparasitic activity against Leishmania donovani.
    Bacopasaponin C
  • HY-N1457
    Chrysosplenetin
    		Inhibitor 99.68%
    Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A.
    Chrysosplenetin
  • HY-132189
    Laniquidar
    		Inhibitor 99.42%
    Laniquidar (R101933) is a noncompetitive, third generation P-glycoprotein (P-gp) inhibitor with an IC50 of 0.51 μM. Laniquidar can be used for modulating multidrug resistance transporters. Laniquidar can also be used for studying acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). Laniquidar has limited oral bioavailability.
    Laniquidar
  • HY-B0947
    Sulfanitran
    		Activator 99.83%
    Sulfanitran is an antibacterial and anticoccidial agent used in poultry feeds. Sulfanitran also is a multidrug resistance protein 2 (MRP2) stimulator that can increase the affinity of MRP2 for estradiol-17-β-D-glucuronide (E217βG).
    Sulfanitran
  • 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-N2947
    Boeravinone B
    		Inhibitor
    Boeravinone B, a dual inhibitor of NorA bacterial efflux pump of Staphylococcus aureus and human P-Glycoprotein, reduces the biofilm formation and intracellular invasion of bacteria. Boeravinone B act as anti-aging and anti-apoptosis phyto-molecules during oxidative stress.
    Boeravinone B
  • HY-N6748
    Roquefortine C
    		Agonist 98.42%
    Roquefortine C is a mycotoxin that can be isolated from Penicillium species. Roquefortine C is an agonist of P-gp and an inhibitor of P450 3A and P450 1A. Roquefortine C can inhibit Gram-positive bacteria and also has certain neurotoxicity. Additionally, Roquefortine C can exert antitumor activity.
    Roquefortine C
  • HY-15134
    ONT-093
    		99.21%
    ONT-093 (OC 144-093) is a potent and orally active inhibitor of P-glycoprotein pump. ONT-093 inhibits P-gp-mediated ATPase activity with an IC50 of 0.16 μM. ONT-093 can inhibit drug efflux and increase bioavailability. ONT-093 reverses cancer cells multidrug resistance to chemotherapeutic drugs. ONT-093 can be used for the researches of cancer and infection, such as colon cancer and malarial .
    ONT-093
  • 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-A0064R
    Verapamil hydrochloride (Standard)
    		Inhibitor
    Verapamil (hydrochloride) (Standard) is the analytical standard of Verapamil (hydrochloride). This product is intended for research and analytical applications. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.
    Verapamil hydrochloride (Standard)
  • HY-123742
    Estradiol 3-sulfate 17-glucuronide potassium
    		Inhibitor 99.92%
    Estradiol 3-sulfate 17-glucuronide potassium is metabolite of estradiol. Estradiol 3-sulfate 17-glucuronide potassium inhibits multidrug resistance protein (MRP) mediated 17β -Estradiol 17-(β -D-Glucuronide) transport with a Ki of 22 μM.
    Estradiol 3-sulfate 17-glucuronide potassium
Cat. No. Product Name / Synonyms Application Reactivity