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-161645
    P-gp modulator-4
    		Modulator
    P-gp modulator-4 (compound 4c) inhibits the efflux function of P-glycoprotein (P-gp). P-gp modulator-4 shows multidrug resistance (MDR) in cancer reversal activity (IC50 of Paclitaxel (HY-B0015) = 8.80, reversal fold = 211.8).
    P-gp modulator-4
  • HY-N2453R
    Convallatoxin (Standard)
    Convallatoxin (Standard) is the analytical standard of Convallatoxin. This product is intended for research and analytical applications. Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties.
    Convallatoxin (Standard)
  • HY-149277
    FM04
    		Inhibitor
    FM04 is a potent P-glycoprotein (P-gp) inhibitor (EC50=83 nM). FM04 inhibits P-gp in 2 mechanism: (1)FM04 binds to Q1193, followed by interacting with the functionally critical residues H1195 and T1226; or (2)FM04 binds to I1115 (a functionally critical residue itself), disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling ICL2-NBD2 interaction and thereby inhibiting P-gp.
    FM04
  • HY-157483
    P-gp inhibitor 18
    		Inhibitor
    P-gp inhibitor 18 (compound 6G) is a potent inhibitor of P-gp. P-gp inhibitor 18 inhibits rhodamine 123 efflux in the P-gp overexpressed leukemia cells, K562/Dox.
    P-gp inhibitor 18
  • HY-10289
    Carmegliptin
    		Modulator
    Carmegliptin (RO-4876904) is an orally active, potent and long-acting dipeptidyl peptidase IV inhibitor. Carmegliptin is also a substrate of P-glycoprotein that synergizes with Verapamil (HY-14275). Carmegliptin improves insulin sensitivity and reduces hepatic glucose production in hyperglycemic mice. Carmegliptin is promising for research of type 2 diabetes, hypertension and cardiovascular disease.
    Carmegliptin
  • HY-144366
    P-gp inhibitor 3
    		Inhibitor
    P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel.
    P-gp inhibitor 3
  • HY-129764A
    (17E)-Prostaglandin F3α
    		Control
    (17E)-Prostaglandin F3α (17-trans-PGF3α) is a double bond isomer of Prostaglandin F3α (HY-129764) and a potential metabolite of trans dietary fatty acids. (17E)-Prostaglandin F3α has anti-inflammatory activity.
    (17E)-Prostaglandin F3α
  • HY-168953
    Lysosomal P-gp targeted agent 1
    		Modulator
    Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume.
    Lysosomal P-gp targeted agent 1
  • HY-161260
    P-gp inhibitor 20
    		Inhibitor
    P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research.
    P-gp inhibitor 20
  • HY-146117
    P-gp modulator 2
    		Modulator
    P-gp modulator 2 (Compound 27) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator.
    P-gp modulator 2
  • HY-N10492
    Spongionellol A analog 1
    		Inhibitor
    Spongionellol A analog 1, an analog of Spongionellol A (HY-10491), is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A analog 1 has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase‑dependent apoptosis. Spongionellol A analog 1 can be used in the research of cancers, such as prostate cancer.
    Spongionellol A analog 1
  • HY-129764
    Prostaglandin F3α
    		Substrate
    Prostaglandin F3α (PGF3α) is an eicosapentaenoic acid (EPA)-derived bioactive lipid mediator that has anti-cancer and anti-inflammatory effects. Prostaglandin F3α is a substrate of ABCC4 with a Km of 12.1 μM. Prostaglandin F3α can be used for the research of diabetes.
    Prostaglandin F3α
  • HY-N144114
    P-gp inhibitor 2
    		Inhibitor
    P-gp inhibitor 2 is a potent P-gp inhibitor. P-gp inhibitor 2 shows reverse Doxorubicin resistance (IC50=0.22 µM) in P-gp overexpressing human colorectal carcinoma cells (SW600 Ad300).
    P-gp inhibitor 2
  • HY-106753
    Tolnapersine
    Tolnapersine exhibits multidrug resistance (MDR) reversal activity, which reverses the resistance of tumor cells to multiple chemotherapy drugs by affecting P-glycoprotein (Pgp) on the cell membrane.
    Tolnapersine
  • HY-155032
    P-gp inhibitor 15
    		Inhibitor
    P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model.
    P-gp inhibitor 15
  • HY-17013D
    Dofequidar sesquifumarate
    		Inhibitor
    Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate 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 sesquifumarate
  • HY-173222
    P-gp inhibitor 28
    		Inhibitor
    P-gp inhibitor 28 (Compound 4h) is an inhibitor targeting P-glycoprotein (P-gp). It can inhibit the proliferation of cancer cells, and its IC50 value for MCF-7/ADR cells is between 15.88 and 21.96 μM. P-gp inhibitor 28 can increase the accumulation of Rho123 in MCF-7/ADR cells and can be used in research related to cancer and overcoming multidrug resistance in tumors.
    P-gp inhibitor 28
  • HY-B0777R
    Moxidectin (Standard)
    Moxidectin (Standard) is the analytical standard of Moxidectin. This product is intended for research and analytical applications. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk.
    Moxidectin (Standard)
  • HY-N10564
    8α,9α-Epoxycoleon-U-quinone
    		Modulator
    8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX.
    8α,9α-Epoxycoleon-U-quinone
  • HY-N0144R
    Piperine (Standard)
    		Inhibitor
    Piperine (Standard) is the analytical standard of Piperine. This product is intended for research and analytical applications. Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC50 of 61.94±0.054 μg/mL.
    Piperine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity