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.

Productos relacionados con P-glycoprotein (356)
Antibodies (3)

By Effects:	Inhibitors (259)

Cat. No.	Nombre del producto	Efecto	Pureza	Chemical Structure

HY-17411

Limonin	Inhibitor	99.38%
Limonin inhibits HIV-1 with an EC₅₀ of 60.0 μM. Limonin induces human colon adenocarcinoma cells apoptosis with an IC₅₀ of 54.74 μM. Limonin has antiviral and antitumor activities.

HY-N0069

Solamargine	Inhibitor	99.87%
Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity.

HY-10550A

Tariquidar methanesulfonate, hydrate	Inhibitor	98.52%
Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a K_d of 5.1 nM.

HY-N0797

(20S)-Protopanaxadiol	Inhibitor	99.94%
20S-protopanaxadiol (aPPD) is a metabolite of ginseng saponins, inhibits Akt activity and induces apoptosis in various tumor cells.

HY-W018791

Bifendate	Inhibitor	99.92%
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).

HY-101453

Ceefourin 1	Inhibitor	99.72%
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.

HY-13646

Encequidar	Inhibitor	99.27%
Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.

HY-B1302

Quinidine hydrochloride monohydrate	Inhibitor	99.97%
Quinidine hydrochloride monohydrate is an orally active antiarrhythmic agent. Quinidine hydrochloride monohydrate reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride monohydrate exerts sustained block and open-channel block effects on I_K(f). Quinidine hydrochloride monohydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride monohydrate can be used in studies related to uterine sarcoma and seizures.

HY-B0532

Trifluoperazine	Inhibitor	99.87%
Trifluoperazine, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine is a potent α1-adrenergic receptor antagonist. Trifluoperazine is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine can be used for the research of schizophrenia. Trifluoperazine acts as a reversible inhibitor of influenza virus morphogenesis.

HY-N3584

Paris saponin VII	Inhibitor	99.84%
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.

HY-N5077

Sinapine	Inhibitor	99.94%
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.

HY-107212

Selamectin	Inhibitor	99.31%
Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, *Lymphatic filariae, and nematode* infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC₅₀ of 120 nM.

HY-N1423A

Glycocholic acid sodium	Inhibitor
Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

HY-N1916

Coniferyl ferulate	Inhibitor	98.73%
Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC₅₀ = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus.

HY-13646A

Encequidar mesylate	Inhibitor	99.82%
Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.

HY-N1423S

Glycocholic acid-d₄	Inhibitor	99.92%
Glycocholic acid-d₄ is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

HY-13687A

IKK 16 hydrochloride	Inhibitor	99.95%
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.

HY-135336

(R)-Verapamil hydrochloride	Inhibitor	99.37%
(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is an orally active P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport. (R)-Verapamil hydrochloride induces Apoptosis and inhibits L-type calcium channels BZPcc, DHPcc and PLLcc. (R)-Verapamil hydrochloride has anti-septic shock and anti-diabetic effects.

HY-N0450

Sinapine thiocyanate	Inhibitor	99.85%
Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.

HY-137433

Befotertinib	Inhibitor	99.86%
Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFR^T790M, EGFR^L858R and delE746-A750, forms covalent bonds with EGFR^C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer.

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P-glycoprotein

P-glycoprotein

Productos relacionados con P-glycoprotein (356)

Antibodies (3)

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