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 Substrates
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P-glycoprotein Ligands
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P-glycoprotein Related Products (379)
Related Products (379)
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Antibodies (3)
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P-gp inhibitor 13
0 ImagesCat. No.: HY-149981CAS No.: 3041121-57-4P-gp inhibitor 13 is a P-gp inhibitor. P-gp inhibitor 13 can reverse P-glycoprotein-mediated paclitaxel resistance in A2780/T cell. P-gp inhibitor 13 can be used for the research of advanced acute myeloid leukemia.
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PGP/FSP1-IN-1
0 ImagesCat. No.: HY-184489CAS No.: 328265-32-3PGP/FSP1-IN-1 is a dual PGP and FSP1 inhibitor and ferroptosis inducer that inhibits the oxidoreductase activity of FSP1. PGP/FSP1-IN-1 competes with NAD (P) H for binding to the pocket of FSP1 and induces FSP1 self-assembly, thereby directly blocking the catalytic function of the relevant enzyme. PGP/FSP1-IN-1 promotes lipid peroxidation and significantly enhances cellular sensitivity to ferroptosis when GPX4 activity is impaired or glutathione synthesis is inhibited. PGP/FSP1-IN-1 can be used in cancer research.
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DHW-221
0 ImagesCat. No.: HY-130133CAS No.: 2378831-21-9DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research.
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(R)-OY-101
0 ImagesCat. No.: HY-149053BCAS No.: 23495-82-1(R)-OY-101 is an orally active and specific inhibitor of P-gp. (R)-OY-101 increases tumor sensitivity to anticancer agents. (R)-OY-101 has good activity in reversing tumor resistance and promoting apoptosis and can be used in cancer related research.
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Solamargine (Standard)
0 ImagesCat. No.: HY-N0069RCAS No.: 20311-51-7Synonyms: Solamargin (Standard); δ-Solanigrine (Standard)Solamargine (Standard) is the analytical standard of Solamargine. This product is intended for research and analytical applications. 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.
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Antibacterial agent 356
0 ImagesCat. No.: HY-184587Antibacterial agent 356 is an orally active antibacterial agent. Antibacterial agent 356 binds to the Mrr1 transcription factor, inhibits the expression of the MDR1 efflux pump gene, reduces the efflux of Rhodamine 123, and increases the accumulation of intracellular substrates in drug-resistant Candida albicans cells. Antibacterial agent 356 induces mitochondrial membrane potential reduction and ROS accumulation in Candida albicans, inhibits the yeast-hypha transition process, and suppresses its biofilm formation. Antibacterial agent 356 reverses efflux pump-mediated drug resistance in azole-resistant Candida albicans with overexpressed Mdr1. Antibacterial agent 356 improves the survival rate of Galleria mellonella larvae infected with azole-resistant Candida albicans*CA632, and reduces the renal fungal load and renal tissue damage in infected BALB/c mice. Antibacterial agent 356 can be used for the research of Candida albicans infection.
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NSC 23925B
0 ImagesCat. No.: HY-117593CAS No.: 1369591-04-7NSC 23925B is a P-glycoprotein (P-gp) inhibitor, as well as the most biologically active isomer of NSC23925 (HY-19626), which reverses and prevents P-glycoprotein-mediated multidrug resistance in cancer cells. NSC 23925B shows weak inhibition against most CYP450 enzymes (IC50 > 10 μM), and exhibits moderate inhibitory activity against CYP2B6 and CYP2D6 with IC50 values of 8.589 μM and 1.407 μM, respectively. NSC 23925B can be used for the research of multidrug-resistant cancers.
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ARN25657
0 ImagesCat. No.: HY-176287ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders.
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P-gp-IN-36
0 ImagesCat. No.: HY-181773P-gp-IN-36 is a potent P-glycoprotein (P-gp) inhibitor with an EC50 of approximately 1 μM. P-gp-IN-36 inhibits the efflux function of P-glycoprotein, overcoming P-gp-mediated multidrug resistance in cancer cells. P-gp-IN-36 inhibits STAT3 phosphorylation and reduces total STAT3 expression. P-gp-IN-36 sensitizes P-gp-expressing cancer cells to the cytostatic effects of conventional cytostatic drugs. P-gp-IN-36 can be used for the research of multidrug-resistant cancer.
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Anticancer agent 108
0 ImagesCat. No.: HY-149240Anticancer agent 108 (Compound 3.10) is a potent P-gp inhibitor with significant antitumor activity and less toxicity to normal and pseudonormal cells. Anticancer agent 108 (Compound 3.10) had no acute toxic effect on С57BL/6 mice.
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PID-9
0 ImagesCat. No.: HY-162369PID-9 is a P-glycoprotein inhibitor. PID-9 has multidrug resistance (MDR) reversal activity (IC50 = 0.1338 μM) and low toxicity. PID-9 inhibits the transport function of P-gp without downregulating P-gp expression.
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Neostenine
0 ImagesCat. No.: HY-N3197CAS No.: 477953-07-4Synonyms: (+)-NeostenineNeostenine is a stenine-type Stemona alkaloid, with antitussive activity. Neostenine is also a substrate of P-glycoprotein with high absorptive permeability in Caco-2 monolayer model. Neostenine also shows oral activity for intestinal application.
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Biricodar dicitrate
0 ImagesCat. No.: HY-13574CAS No.: 174254-13-8Synonyms: VX 710-3Biricodar dicitrate (VX 710-3) is the dicitrate salt form of Biricodar (HY-13574A). Biricodar dicitrate is an inhibitor for P-glycoprotein and multidrug resistance-associated protein 1 (MRP-1), which increases the accumulation of chemotherapy drugs within cancer cells and shows effective chemosensitizing activity in multidrug resistant cells.
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P-gp inhibitor 24
0 ImagesCat. No.: HY-159085P-gp inhibitor 24 (Compound 10) is an inhibitor for P-glycoprotein (P-gp)), that inhibits the P-gp mediated fluorescent dye efflux. P-gp inhibitor 24 exhibits multidrug resistance (MDR) reversal effect, enhances the cytotoxicity of Vincristine (HY-N0488) and Etoposide (HY-13629) in cancer cells.
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2-Propylpent-4-ynoic acid
0 ImagesCat. No.: HY-W787758CAS No.: 24102-11-2Synonyms: 4-yn-VPA2-Propylpent-4-ynoic acid (4-yn-VPA) is a HDAC inhibitor (with an IC50 of 0.5 mM against human HDAC). 2-Propylpent-4-ynoic acid also induces P-glycoprotein function, and exhibits teratogenicity, fetal growth inhibition and neurotoxicity. 2-Propylpent-4-ynoic acid shows significant stereospecific teratogenic effects, with the S-enantiomer being more teratogenic than the R-enantiomer and other analogs. The neurotoxicity of 2-Propylpent-4-ynoic acid is independent of its stereochemical structure. 2-Propylpent-4-ynoic acid has been used in studies related to the pathogenesis of colon cancer and neural tube defects such as exencephaly.
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Trifluoperazine-d3 dihydrochloride
0 ImagesCat. No.: HY-B0532ASCAS No.: 1432064-02-2Trifluoperazine-d3 (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
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Tyroservatide
0 ImagesCat. No.: HY-106035CAS No.: 154039-16-4Synonyms: YSVTyroservatide (YSV) is an active, low-molecular-weight polypeptide that has been shown to have antitumor effects on hepatocellular carcinoma and lung cancer cell.
