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-150565
    P-gp inhibitor 5
    		Inhibitor
    P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-InTM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015).
    P-gp inhibitor 5
  • 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-N2947R
    Boeravinone B (Standard)
    		Inhibitor
    Boeravinone B (Standard) is the analytical standard of Boeravinone B. This product is intended for research and analytical applications. 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 (Standard)
  • HY-149360
    P-gb-IN-1
    		Inhibitor
    P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells.
    P-gb-IN-1
  • HY-149813
    P-gp inhibitor 14
    		Inhibitor
    P-gp inhibitor 14 (Compound 8a) is a high affinity P-gp inhibitor. P-gp inhibitor 14 reverses P-gp-mediated multidrug resistance (EC50=48.74 nM). P-gp inhibitor 14 has a weak inhibitory effect on CYP3A4 activity.
    P-gp inhibitor 14
  • HY-11018R
    Risperidone (Standard)
    		Inhibitor
    Risperidone (Standard) is the analytical standard of Risperidone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-168921
    ABCB1-IN-3
    		Inhibitor
    ABCB1-IN-3 (Compound K27) is an orally active inhibitor of ABCB1, and induces apoptosis. ABCB1-IN-3 directly binds to ABCB1 to inhibit efflux function, ensuring stable intracellular concentration of Paclitaxel (PTX) (HY-B0015) without affecting ABCB1 normal expression. ABCB1-IN-3 significantly increases the sensitivity of ABCB1-mediated multidrug resistance (MDR) to PTX in vitro, enhances cell cycle arrest, and inhibits proliferation. BCB1-IN-3 combined with PTX exhibits potent tumor suppression in vivo without generating toxicity.
    ABCB1-IN-3
  • HY-157484
    P-gp inhibitor 19
    		Inhibitor
    P-gp inhibitor 19 (Compound 6i) is a P-gp inhibitor. P-gp inhibitor 19 can inhibit the efflux of rhodamine 123 (HY-D0816) in P-gp-overexpressing leukemia cells K562/Dox and also restore the sensitivity of DOX-resistant cells.
    P-gp inhibitor 19
  • HY-N5077B
    Sinapine hydroxide
    		Inhibitor
    Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
    Sinapine hydroxide
  • HY-13776A
    XR9051 hydrochloride
    		Modulator
    XR9051 hydrochloride is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR).
    XR9051 hydrochloride
  • HY-157330
    P-gp inhibitor 16
    		Inhibitor
    P-gp inhibitor 16 (compound 14) is a p-glycoprotein inhibitor. P-gp inhibitor 16 significantly increases Doxorubicin-induced apoptosis and shows anticancer effects.
    P-gp inhibitor 16
  • HY-162447
    P-gp inhibitor 22
    		Inhibitor
    P-gp inhibitor 22 is a P-glycoprotein (P-gp) inhibitor that effectively inhibits P-pg and efflux function. P-gp inhibitor 22 induces apoptosis and accumulation of MCF-7/ADR cells processed in the S phase.
    P-gp inhibitor 22
  • HY-W009141R
    1-Monopalmitin (Standard)
    		Inhibitor
    1-Monopalmitin (Standard) is the analytical standard of 1-Monopalmitin. This product is intended for research and analytical applications. 1-Monopalmitin, a bitter melon extract, inhibits the P-glycoprotein (P-gp) activity in intestinal Caco-2 cells.
    1-Monopalmitin (Standard)
  • HY-B0532AR
    Trifluoperazine (dihydrochloride) (Standard)
    		Inhibitor
    Trifluoperazine (dihydrochloride) (Standard) is the analytical standard of Trifluoperazine (dihydrochloride). This product is intended for research and analytical applications. Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine (dihydrochloride) (Standard)
  • HY-11018S1
    Risperidone-d4-1
    		Inhibitor
    Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). 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>-1
  • 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-162396
    P-gp inhibitor 21
    		Inhibitor
    P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity.
    P-gp inhibitor 21
  • HY-P990196
    Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2)
    		Inhibitor
    Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) is a mouse-derived IgG2a, κ type antibody inhibitor, targeting to monkey/human MDR-1/CD243.
    Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2)
  • 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)
Cat. No. Product Name / Synonyms Application Reactivity