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 (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.
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P-glycoprotein Inhibitors
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P-glycoprotein Ligands
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P-glycoprotein Related Products (381)
Related Products (381)
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Antibodies (3)
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Cajanol
0 ImagesCat. No.: HY-N10342CAS No.: 61020-70-0Cajanol is an isoflavanone that can be isolated from the roots of Cajanus cajan (L.) Millsp.. Cajanol inhibits cancer cell proliferation and induces cancer cell apoptosis. Cajanol promotes the expression of Bax, inhibits the expression of Bcl-2, activates caspase-9 and caspase-3, induces PARP cleavage, arrests the cell cycle at the G2/M phase, generates ROS, disrupts mitochondrial membrane potential and triggers cytochrome c release. Cajanol induces bacterial DNA damage, disrupts bacterial cell membranes, and exerts antibacterial activity in vitro. Cajanol reduces the expression of PI3K, inhibits the phosphorylation of Akt and NF-κB, downregulates the expression and transport function of P-gp, restores the sensitivity of drug-resistant cancer cells to Paclitaxel, and inhibits the growth of Paclitaxel-resistant metastatic ovarian tumors. Cajanol is applicable to research related to breast cancer, ovarian cancer and bacterial infections.
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P-gp inhibitor 3
0 ImagesCat. No.: HY-144366CAS No.: 2766451-11-8P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel.
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(17E)-Prostaglandin F3α
0 ImagesCat. No.: HY-129764ACAS No.: 211100-24-2Synonyms: 17-trans-PGF3α(17E)-Prostaglandin F3α (17-trans-PGF3α) is a double bond isomer of Prostaglandin F3α (HY-129764) and a potential metabolite of trans dietary fatty acids. (17E)-Prostaglandin F3α has anti-inflammatory activity.
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Lysosomal P-gp targeted agent 1
0 ImagesCat. No.: HY-168953CAS No.: 3043797-88-9Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume.
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P-gp inhibitor 20
0 ImagesCat. No.: HY-161260CAS No.: 3040917-33-4P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research.
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P-gp modulator 2
0 ImagesCat. No.: HY-146117CAS No.: 2987145-05-9P-gp modulator 2 (Compound 27) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator.
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P-gp inhibitor 29
0 ImagesCat. No.: HY-173401CAS No.: 3082344-99-5P-gp inhibitor 29 (41) is a highly potent P-gp inhibitor and apoptosis inducer, with an IC50 of 8.9 nM in Eca109/VCR cells. P-gp inhibitor 29 (41) can be used in the research for Esophageal Cancer.
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BMS 275183
0 ImagesCat. No.: HY-106219CAS No.: 355113-98-3BMS 275183 is a potent, orally active analogue of Paclitaxel (HY-B0015). BMS 275183 can stabilize microtubules and exhibits antitumor activity in in vivo tumor models. BMS 275183 is active in vitro against Paclitaxel-resistant tumors including those harboring tubulin mutations or overexpressing P-glycoprotein. BMS 275183 can be used for cancer research, such as non-small cell lung cancer (NSCLC) and prostate carcinoma.
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P-gp-IN-32
0 ImagesCat. No.: HY-175838CAS No.: 2918249-59-7P-gp-IN-32 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-32 exhibits low cytotoxicity and potent multidrug resistance (MDR) reversal activity against Doxorubicin (HY-15142A) in MCF7/ADR cells (IC50 = 0.11 μM, reversal fold (RF) = 215.9). P-gp-IN-32 can bind to P-gp directly, induce a conformation change of P-gp and inhibit the efflux function. P-gp-IN-32 can be used for the research of cancer, such as breast cancer.
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Spongionellol A analog 1
0 ImagesCat. No.: HY-N10492Spongionellol A analog 1, an analog of Spongionellol A (HY-10491), is a MDR1 (p-glycoprotein) inhibitor. Spongionellol A analog 1 has high cytotoxic activity and selectivity in prostate cancer cells by inducing caspase?dependent apoptosis. Spongionellol A analog 1 can be used in the research of cancers, such as prostate cancer.
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CP-100356
0 ImagesCat. No.: HY-108347ACAS No.: 142716-85-6CP-100356 is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 is also a weak inhibitor of OATP1B1 (IC50 = ∼66 µM). CP-100356 is devoid of inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM).
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Prostaglandin F3α
0 ImagesProstaglandin F3α (PGF3α) is an eicosapentaenoic acid (EPA)-derived bioactive lipid mediator that has anti-cancer and anti-inflammatory effects. Prostaglandin F3α is a substrate of ABCC4 with a Km of 12.1 μM. Prostaglandin F3α can be used for the research of diabetes.
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BRAFV600E/ABL2-IN-2
0 ImagesCat. No.: HY-181726BRAFV600E/ABL2-IN-2 is a dual BRAFV600E and ABL2 kinase inhibitor, with an IC50 of 0.088 μM against human BRAFV600E and an IC50 of 0.3 μM against human ABL2. BRAFV600E/ABL2-IN-2 reduces the phosphorylation levels of downstream ERK1/2 and CrkL in melanoma cells. BRAFV600E/ABL2-IN-2 decreases the expression of P-glycoprotein (P-glycoprotein) in melanoma cells. BRAFV600E/ABL2-IN-2 induces G1 cell cycle arrest and apoptosis (Apoptosis) in melanoma cells. BRAFV600E/ABL2-IN-2 is applicable to relevant research on melanoma.
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Roquefortine C-13C22
0 ImagesCat. No.: HY-N6748SRoquefortine C-13C22 is the 13C-labeled Roquefortine C (HY-N6748). Roquefortine C is a mycotoxin that can be isolated from Penicillium species. Roquefortine C is an agonist of P-gp and an inhibitor of P450 3A and P450 1A. Roquefortine C can inhibit Gram-positive bacteria and also has certain neurotoxicity. Additionally, Roquefortine C can exert antitumor activity.
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C2 Adamantanyl globotriaosylceramide (d18:1/2:0)
0 ImagesCat. No.: HY-156207CAS No.: 261155-87-7Synonyms: AdaGb3; Adamantyl Gb3; C2 Adamantanyl Ceramide Trihexoside (d18:1/2:0)C2 Adamantanyl globotriaosylceramide (d18:1/2:0) (AdaGb3), a water-soluble globotriaosylceramide analog, is a bioactive sphingolipid. C2 Adamantanyl globotriaosylceramide (d18:1/2:0) reverses MDR1-MDCK cell drug resistance. C2 Adamantanyl globotriaosylceramide (d18:1/2:0) has high affinity for verotoxin (VT).
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S 16317
0 ImagesCat. No.: HY-120790CAS No.: 151489-04-2S 16317 is an orally active dihydropyridine derivative with low calcium channel affinity (Ki: 0.55 μM). S 16317 inhibits P-gp mediated efflux of ADR. S 16317 overcomes multidrug resistance in tumor.
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P-gp inhibitor 2
0 ImagesCat. No.: HY-N144114CAS No.: 2408406-89-1P-gp inhibitor 2 is a potent P-gp inhibitor. P-gp inhibitor 2 shows reverse Doxorubicin resistance (IC50=0.22 µM) in P-gp overexpressing human colorectal carcinoma cells (SW600 Ad300).
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Tolnapersine
0 ImagesCat. No.: HY-106753CAS No.: 70312-00-4Tolnapersine exhibits multidrug resistance (MDR) reversal activity, which reverses the resistance of tumor cells to multiple chemotherapy drugs by affecting P-glycoprotein (Pgp) on the cell membrane.
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P-gp inhibitor 15
0 ImagesCat. No.: HY-155032CAS No.: 2303508-09-8P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model.
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Dofequidar sesquifumarate
0 ImagesCat. No.: HY-17013DCAS No.: 158681-49-3Synonyms: MS-209 sesquifumarateDofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate 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.
