- Signaling Pathways
- Membrane Transporter/Ion Channel
- 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
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P-glycoprotein Inhibitors
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P-glycoprotein Ligand
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P-glycoprotein Related Products (375)
Related Products (375)
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Antibodies (3)
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Befotertinib
0 ImagesSynonyms: D-0316Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFRT790M, EGFRL858R and delE746-A750, forms covalent bonds with EGFRC797, 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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Sinapine thiocyanate
0 ImagesSinapine 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. -
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Glycocholic acid (Standard)
0 ImagesGlycocholic acid (Standard) is the analytical standard of Glycocholic acid (HY-N1423). This product is intended for research and analytical applications. Glycocholic acid is a bile acid with anticancer activity, targeting against pump resistance-related and non-pump resistance-related pathways. -
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Indican
0 ImagesIndican (Indoxyl-β-D-glucoside), a glycoside of indoxyl, is a precursor of the dyesindigo and indirubin. Indican has a major metabolite, indoxyl sulfate (IS). IS, an uremic toxin, is a substrate/inhibitor of organic anion transporter (OAT) 1, OAT 3 and multidrug resistance-associated protein (MRP) 4. -
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Norverapamil hydrochloride
0 ImagesSynonyms: (±)-Norverapamil hydrochloride; D591 hydrochlorideNorverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor. -
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TTT-28
0 ImagesTTT-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. -
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Poloxamer 403 (P123)
0 ImagesCat. No.: HY-D1005A25CAS No.: 9003-11-6Synonyms: PEG-PPG-PEG, 5750 (Average)Poloxamer 403 P123 is a block copolymer of polyoxyethylene and polyoxypropylene with an average molecular weight of 5750. Poloxamer has the ability to inhibit P-gp. Poloxamer 403 increases creatine kinase levels. Poloxamer 403 is myotoxic. -
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Furanodiene
0 ImagesFuranodiene 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. -
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Bisdemethoxycucurmin
0 ImagesSynonyms: Curcumin III; DidemethoxycurcuminBisdemethoxycucurmin (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. -
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Dofequidar fumarate
0 ImagesSynonyms: MS-209Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate 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. -
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Isosinensetin
0 ImagesIsosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC50: 2.61 µM; Ki: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc. -
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ZW-1226
0 ImagesZW-1226 is a dual Tyrosyl DNA phosphodiesterase 2 (TDP2) and Multidrug resistance-associated protein 1 (MRP1) inhibitor with IC50 values of 0.2 and 0.5 μM, respectively. ZW-1226 exhibits selectivity over other ABC transporters. ZW-1226 elevates intracellular GSH levels, and reverses MRP1-mediated drug resistance. ZW-1226 can be used for the research of leukemia, non-small-cell lung cancer, and multidrug resistant small-cell lung cancer. -
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Glyburide-d3
0 ImagesSynonyms: Glyburide-d3Glyburide-d3 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[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5]. -
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Zamicastat
0 ImagesSynonyms: BIA 5-1058Zamicastat (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. -
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1-Monopalmitin
0 ImagesSynonyms: Glyceryl palmitate1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC50=50-58 μg/mL), with low toxicity to normal cells. -
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LY-402913
0 ImagesLY-402913 is a selective multidrug resistance protein (MRP1) inhibitor. -
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Poloxamer 184 (L64)
0 ImagesCat. No.: HY-D1005A10CAS No.: 9003-11-6Synonyms: PEG-PPG-PEG, 2900 (Average)Poloxamer 184 L64 is a block copolymer of polyethylene oxide and polypropylene oxide with an average molecular weight of 2900. Poloxamer has the ability to inhibit P-gp. Poloxamer 184 exhibits short-term skin toxicity, characterized by mild erythema and intradermal inflammatory reactions. Poloxamer 184 has antimicrobial activity, inhibiting 60% of Mycobacterium avium at a concentration of 1 mg/mL. Poloxamer 184 forms a thermoreversible hydrogel and is used as a food additive and as a drug delivery carrier in cosmetics and tissue engineering. -
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Dofequidar
0 ImagesSynonyms: MS-209 free baseDofequidar (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. -
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Verapamil-d3 hydrochloride
0 ImagesCat. No.: HY-A0064SCAS No.: 2714485-49-9Synonyms: (±)-Verapamil-d3 hydrochloride; CP-16533-1-d3 hydrochlorideVerapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. 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. -
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Polyphyllin H
0 ImagesPolyphyllin H is a steroidal saponin. Polyphyllin H is isolated from Paris polyphylla. Polyphyllin H potently inhibits the activities of CYP1A2 (IC50 = 6.44 μM, competitive), CYP2D6 (IC50 = 13.88 μM, competitive) and CYP3A4 (IC50 = 4.52 μM, non-competitive, time-dependent). Polyphyllin H downregulates the expression of ABCB1 and ABCC3. Polyphyllin H binds to membrane cholesterol and disrupts lipid raft structures. Polyphyllin H restores the sensitivity of paclitaxel-resistant breast cancer cells to paclitaxel. -
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