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-126940
    Furanodiene
    		Inhibitor 99.65%
    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-139848
    WS-898
    		Inhibitor 98.14%
    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-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-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-132866
    YS-370
    		Inhibitor 98.50%
    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-N0689
    Evodine
    		Inhibitor 99.20%
    Evodine, the major limonoid of Evodiae Fuctus, is a potent P-gp inhibitor. Evodine has protection against glutamateinduced toxicity by preserving the antioxidant defense system.
    Evodine
  • 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-B0501
    Danofloxacin mesylate
    		99.87%
    Danofloxacin mesylate (CP 76136-27) is a fluoroquinolone used as a veterinary drug. Danofloxacin mesylate has a broad spectrum of bactericidal activity, mainly inhibiting the DNA cycloenzyme of the bacteria. In addition, Danofloxacin mesylate is a substrate for ATP-dependent efflux transporters (P-gp and MRP2).
    Danofloxacin mesylate
  • HY-13574A
    Biricodar
    		Modulator 99.31%
    Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
    Biricodar
  • HY-N6748
    Roquefortine C
    		Activator 98.42%
    Roquefortine C, a fungal cyclopeptide isolated from Penicillium roquefortii, activates P-gp and also inhibits P450-3A and other haemoproteins. Roquefortine C has bacteriostatic activities against Gram-positive bacteria.
    Roquefortine C
  • HY-132189
    Laniquidar
    		Inhibitor
    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-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-110232
    Risperidone-d4
    		Inhibitor 99.40%
    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-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-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 a potent and orally active huntingtin (HTT) splicing modulator. HTT-D3 acts by promoting the inclusion of a pseudoexon containing a premature termination codon (stop-codon psiExon), leading to HTT mRNA degradation and reduction of HTT levels. HTT-D3 reduces p-glycoprotein (P-gp) efflux, and can be uesd for Huntington's disease research.
    HTT-D3
  • HY-123742
    Estradiol 3-sulfate 17-glucuronide potassium
    		Inhibitor 98.33%
    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
  • HY-N0406
    2"-O-beta-L-galactopyranosylorientin
    		99.96%
    2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2). Anti-inflammatory effect.
    2
  • 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
Cat. No. Product Name / Synonyms Application Reactivity