Home Transmembrane Transporters P-gp

P-gp

P-glycoprotein (permeability glycoprotein, P-gp, Pgp, ABCB1, ATP-binding cassette sub-family B member 1, MDR1, and PGY1) is belongs to a subfamily of ABC-transporter called MDR (Classical multidrug resistance). P-glycoprotein functions as a transporter in the blood-brain barrier with a 170 kDa polypeptide. P-gp plays a role in the elimination of drugs and metabolites in kidney and liver, and these cumulative systemic effects would eventuate in lower plasma concentrations of these drugs. P-gp inhibitors can be a kind of anti-cancer drug through reducing multidrug resistance because P-glycoprotein (Pgp), the membrane-associated protein, is overexpressed in tumor cells resulting in an enhanced ability to export drugs from the cell and multidrug resistance.

Other Transmembrane Transporters Related Inhibitors

CFTR CRM1 Calcium Channel Proton Pump Sodium Channel ATPase Potassium Channel CD markers GLUT Amino acid transporter
Cat.No. Product Name Information Product Use Citations Product Validations
S8028 Tariquidar (XR9576) Tariquidar is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM in CHrB30 cell line, reverses drug resistance in MDR cell Lines. Phase 3.
Journal of Medicinal Chemistry, November 18 2025, 23962-23976
Anticancer Research, March 15 2023, 1103-1112
Molecular Cancer Therapeutics, July 05 2022, 1227-1235
Verified customer review of Tariquidar (XR9576)
S1481 Zosuquidar 3HCl Zosuquidar 3HCl is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM in a cell-free assay. Phase 3.
Acta Pharmacol Sin, 2026, 10.1038/s41401-026-01791-z
bioRxiv, 2025, 2025.06.18.660465
Hepatol Commun, 2024, 8(5)e0437
Verified customer review of Zosuquidar 3HCl
S7772 Elacridar (GF120918) Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.
Acta Pharmacol Sin, 2026, 10.1038/s41401-026-01791-z
Nat Commun, 2025, 16(1):5511
Cell Rep Med, 2025, 6(6):102160
Verified customer review of Elacridar (GF120918)
E1781 Biricodar Biricodar(VX-710) is a modulator of P-glycoprotein and MRP-1 with minimal in vivo toxicity. It enhances the effectiveness of various antibiotics against numerous gram-positive pathogens and exhibits potent chemosensitizing properties in cells resistant to multiple drugs.
Cancer Discov, 2026, 10.1158/2159-8290.CD-25-1459
S4746 (20S)-Protopanaxadiol 20(S)-Protopanaxadiol (PPD, 20-Epiprotopanaxadiol), the main intestinal metabolite of ginsenosides, is one of the active ingredients in ginseng. 20(S)-Protopanaxadiol inhibits P-glycoprotein in multidrug resistant cancer cells.
Front Pharmacol, 2025, 16:1530270
E0080 UCLA GP130 2 UCLA GP130 2 (GP130 receptor agonist-1) is a potent, brain-penetrant and orally active Glycoprotein 130 (Gp130) receptor agonist, being a humanin mimetic binding to the GP130 D4-D5 domain and reducing NMDA-induced toxicity.
Molecular Medicine Reports, March 7, 2025, 121
S9145 Solamargine Solamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition.
Sci Rep, 2016, 6:36721
S3235 Sinapine Sinapine is an alkaloid isolated from seeds of the cruciferous species with antioxidant, antitumor and radio-protective activities. This compound inhibits the proliferation of Caco-2 cells via downregulation of P-glycoprotein.
Gene, 2022, 827:146460
E1742 Reversan Reversan (CBLC4H10) is a selective and nontoxic inhibitor of multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (P-gp), with the potential to treat neuroblastoma and other MRP1-overexpressing drug-refractory tumors.
Cancer Discov, 2026, 10.1158/2159-8290.CD-25-1459
S0921 Wilforine Wilforine (WR), a sesquiterpene pyridine alkaloid found in T. wilfordii plants, significantly inhibits the efflux activity of P-glycoprotein (P-gp).

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