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-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-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
  • 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-N0406
    2"-O-beta-L-galactopyranosylorientin
    		99.91%
    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-126906
    Milbemycin A4
    		Inhibitor 99.13%
    Milbemycin A4 inhibits P-glycoprotein activity, and reverses multidrug resistance of tumor cells. Milbemycins are a family of macrolide antibiotics with insecticidal and acaricidal activitysup>[2].
    Milbemycin A4
  • HY-N0797R
    (20S)-Protopanaxadiol (Standard)
    		Inhibitor
    (20S)-Protopanaxadiol (Standard) is the analytical standard of (20S)-Protopanaxadiol. This product is intended for research and analytical applications. 20S-protopanaxadiol (aPPD) is a metabolite of ginseng saponins, inhibits Akt activity and induces apoptosis in various tumor cells.
    (20S)-Protopanaxadiol (Standard)
  • HY-B0777S
    Moxidectin-d3
    Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. 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-d<sub>3</sub>
  • HY-19626
    NSC23925
    		Inhibitor 99.43%
    NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor.
    NSC23925
  • HY-15206S
    Glyburide-d11
    		Inhibitor 99.39%
    Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.
    Glyburide-d<sub>11</sub>
  • 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-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-N1514
    Ganoderenic acid B
    		99.95%
    Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin.
    Ganoderenic acid B
  • 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-N11424
    Bilirubin diglucuronide
    		Inhibitor
    Bilirubin diglucuronide is the metabolite of Bilirubin (HY-N0323). Bilirubin diglucuronide inhibits MRP1/2 mediated ATP-dependent transport of leukotriene C4 (LTC4) in membrane vesicles.
    Bilirubin diglucuronide
  • 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-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-155391
    hCA/Wnt/β-catenin-IN-1
    		Inhibitor 99.96%
    hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor of hCA (Ki: 33.6, 24.1, 6.8 nM for hCA II, hCA IX, hCA XII). hCA/Wnt/β-catenin-IN-1 reduces P-gp activity. hCA/Wnt/β-catenin-IN-1 also inhibits Wnt/β-catenin signaling pathway. hCA/Wnt/β-catenin-IN-1 inhibits cancer cell viability, including the NCI/ADR-RES DOX-resistant cell line.
    hCA/Wnt/β-catenin-IN-1
  • 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-148574
    MCT1-IN-3
    		98.65%
    MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC50 value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer.
    MCT1-IN-3
  • HY-N0007AR
    Bisdemethoxycucurmin (Standard)
    		Inhibitor
    Bisdemethoxycucurmin (Standard) (Curcumin III (Standard)) is the analytical standard of Bisdemethoxycucurmin (HY-N0007A). This product is intended for research and analytical applications. Bisdemethoxycucurmin (Curcumin III) is a curcuminoid compound and an inhibitor of P-glycoprotein and ferroptosis. Bisdemethoxycucurmin exhibits multiple activities such as anti-oxidation, anti-inflammation and anti-tumor. Bisdemethoxycucurmin can be used for the research of tumors and inflammatory diseases.
    Bisdemethoxycucurmin (Standard)
Cat. No. Product Name / Synonyms Application Reactivity