- 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 Substrates
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P-glycoprotein Ligands
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P-glycoprotein Related Products (385)
Related Products (385)
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Antibodies (3)
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SC209
0 ImagesSynonyms: 3-Aminophenyl HemiasterlinSC209 (3-Aminophenyl Hemiasterlin) is a 3-aminophenyl hemiasterlin derivative that serves as a cytotoxin for ADCs, targeting tubulin. SC209 has reduced potential for drug efflux via P-glycoprotein 1 drug pump compared with other tubulin-targeting payloads. SC209 exhibits antitumor activity and can be used in the synthesis of ADC molecules. -
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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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Biricodar
0 ImagesSynonyms: VX-710Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells. -
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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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Tenacissoside G
0 ImagesTenacissoside G is a C21 steroidal glycoside. Tenacissoside G inhibits Src and NF-κB, downregulates the activities of PTN and P-gp, induces DNA damage and apoptosis in cancer cells, inhibits their proliferation and migration, and reverses the resistance of ovarian cancer cells to Paclitaxel (HY-B0015). Tenacissoside G inhibits the expression of iNOS, TNF-α, IL-6, MMP-3, and MMP-13, reduces type II collagen degradation, and alleviates articular cartilage damage. Tenacissoside G can be used in studies related to ovarian cancer, colorectal cancer, and osteoarthritis. -
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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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Sodium glycocholate hydrate, 98%
0 ImagesSynonyms: N-Cholylglycine sodium salt, 98%Sodium glycocholate hydrate, 98% is a bile acid derivative. Sodium glycocholate hydrate, 98% downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Sodium glycocholate hydrate, 98% inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Sodium glycocholate hydrate, 98% modulates related bile acid receptor signaling. Sodium glycocholate hydrate, 98% suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Sodium glycocholate hydrate, 98% can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA). -
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CPI1
0 ImagesCPI1 is a multidrug resistance protein 1 (MRP1) inhibitor with a Ki value of 100 nM. CPI1 binds to the same substrate-binding site as leukotriene C4, stabilizes MRP1 in an apo-like inward-facing conformation, blocks the conformational changes required for ATP hydrolysis and substrate transport, and inhibits the ATPase activity of human and bovine MRP1. CPI1 serves as a tool for investigating the substrate transport mechanism of MRP1. CPI1 is applicable to research related to cancer multidrug resistance. -
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GPV0057
0 ImagesGPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome. -
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