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.
Nat Commun, 2025, 16(1):5511
J Transl Med, 2025, 23(1):542
Cells, 2025, 14(16)1276
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.
bioRxiv, 2025, 2025.06.18.660465
Hepatol Commun, 2024, 8(5)e0437
Adv Healthc Mater, 2022, e2201984
Verified customer review of Zosuquidar 3HCl
S7772 Elacridar (GF120918) Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.
Nat Commun, 2025, 16(1):5511
Cell Rep Med, 2025, 6(6):102160
Nanoscale, 2025, 17(16):9947-9962
Verified customer review of Elacridar (GF120918)
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
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
S0921 Wilforine Wilforine (WR), a sesquiterpene pyridine alkaloid found in T. wilfordii plants, significantly inhibits the efflux activity of P-glycoprotein (P-gp).
S3431 Encequidar (HM30181) Encequidar (HM30181, HM30181A) is a potent and selective inhibitor of the adenosine triphosphate-binding cassette transporter P-glycoprotein (P-gp).
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.
S8130New Valspodar Valspodar is a second-generation, non-immunosuppressive inhibitor of P-glycoprotein (Pgp) that reverses multidrug resistance by blocking drug efflux. It enhances the intracellular accumulation of chemotherapeutics like mitoxantrone, restoring drug sensitivity in resistant cancer cells.

Signaling Pathway Map