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-11018B
    Risperidone mesylate
    		Inhibitor
    Risperidone mesylate(R 64 766 mesylate) 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 mesylate
  • HY-169782
    CJZ3
    		Inhibitor
    CJZ3 is an reversible inhibitor for P-glycoprotein (P-gp), that accumulates the drug (Rh123) in cells, and improve the permeability of the blood-brain barrier (BBB).
    CJZ3
  • HY-50671R
    Zosuquidar trihydrochloride (Standard)
    		Inhibitor
    Zosuquidar (trihydrochloride) (Standard) is the analytical standard of Zosuquidar (trihydrochloride). This product is intended for research and analytical applications. Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research.
    Zosuquidar trihydrochloride (Standard)
  • HY-W018791R
    Bifendate (Standard)
    		Inhibitor
    Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR).
    Bifendate (Standard)
  • HY-101511R
    TTT-28 (Standard)
    		Inhibitor
    TTT-28 (Standard) is the analytical standard of TTT-28 (HY-101511). This product is intended for research and analytical applications. TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.
    TTT-28 (Standard)
  • HY-107643R
    Reversan (Standard)
    		Inhibitor
    Reversan (Standard) is the analytical standard of Reversan (HY-107643). This product is intended for research and analytical applications. Reversan (CBLC4H10) inhibits drug efflux mediated by P-glycoprotein (Pgp) and multidrug resistance protein 1 (MRP1), and exhibits oral activity. Reversan shows activity against glioblastoma multiforme and neuroblastoma models.
    Reversan (Standard)
  • HY-13646R
    Encequidar (Standard)
    		Inhibitor
    Encequidar (Standard) is the analytical standard of Encequidar. This product is intended for research and analytical applications. Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.
    Encequidar (Standard)
  • HY-15206S2
    Glibenclamide-13C6
    		Inhibitor
    Glibenclamide-13C6 (Glyburide-13C6) is 13C 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.
    Glibenclamide-<sup>13</sup>C<sub>6</sub>
  • HY-106265
    9,10-trans-Dehydroepothilone D
    		Inhibitor
    9,10-trans-Dehydroepothilone D shows an antiproliferative activity against a paclitaxel-resistant cell lines overexpressing P-glycoprotein. 9,10-trans-Dehydroepothilone D also shows tubulin polymerization activity. 9,10-trans-Dehydroepothilone D is given by lactonization of Seco acid, which is promising for research of cancers.
    9,10-trans-Dehydroepothilone D
  • HY-174454
    Antitrypanosomal agent 24
    		Inhibitor
    Antitrypanosomal agent 24 is a benzothiazole amidoxime with strong and selective antitrypanosomal activity (IC50 = 0.92 μM). Antitrypanosomal agent 24 is a substrate of the P-glycoprotein efflux pump. Antitrypanosomal agent 24 has high membrane permeability and good metabolic stability. Antitrypanosomal agent 24 binds to DNA/RNA by intercalation.
    Antitrypanosomal agent 24
  • HY-N15297
    Isotenulin
    		Inhibitor
    Isotenulin inhibits the efflux function of P-glycoprotein by stimulation of P-glycoprotein ATPase, thereby overcoming the multidrug resistance (MDR) of cancer cells. Isotenulin exhibits cytotoxicity in multidrug-resistant cancer cell KB-vin and sensitive cancer cell HeLaS3. Isotenulin exhibits synergistic effect with Paclitaxel (HY-B0015), Vinblastine (HY-13780) and Doxorubicin (HY-15142).
    Isotenulin
  • HY-13687R
    IKK 16 (Standard)
    		Inhibitor
    IKK 16 (Standard) is the analytical standard of IKK 16. This product is intended for research and analytical applications. IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.
    IKK 16 (Standard)
  • HY-101453R
    Ceefourin 1 (Standard)
    		Inhibitor
    Ceefourin 1 (Standard) is the analytical standard of Ceefourin 1 (HY-101453). This product is intended for research and analytical applications. Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma.
    Ceefourin 1 (Standard)
  • HY-W654320
    Piperin-d10
    		Inhibitor
    Piperin-d10 is deuterium labeled Piperine. 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.
    Piperin-d<sub>10</sub>
  • HY-N5077R
    Sinapine (Standard)
    		Inhibitor
    Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine 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 (Standard)
  • HY-107197
    8-Prenylchrysin
    		Inhibitor
    8-prenylchrysin is a C8-prenylated flavonoid. 8-prenylchrysin inhibits P-gp. 8-prenylchrysin can be used for tumor research.
    8-Prenylchrysin
  • HY-N7332
    Pepluanin A
    		Inhibitor
    Pepluanin A is a natural compound isolated from Euphorbia peplus L. Pepluanin A shows a very high activity for a jatrophane diterpene, outperforming Cyclosporin A by a factor of at least 2 in the inhibition of Pgp-mediated Daunomycin (HY-13062A) transport[1]
    Pepluanin A
  • HY-106004R
    Zamicastat (Standard)
    		Inhibitor
    Zamicastat (Standard) is the analytical standard of Zamicastat (HY-106004). This product is intended for research and analytical applications. 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 (Standard)
  • HY-N11084
    Salviaplebeiaside
    		Inhibitor
    Salviaplebeiaside is a phenolic substance can be isolated from the aerial part of Vitex negundo var. cannabifolia. Salviaplebeiaside is an inhibitor of class I p-glycoprotein.
    Salviaplebeiaside
  • HY-14275S
    Verapamil-d3
    		Inhibitor
    Verapamil-d3 ((±)-Verapamil-d3) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.
    Verapamil-d<sub>3</sub>
Cat. No. Product Name / Synonyms Application Reactivity