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.

Transmembrane Transporters

CGRP Receptor Endothelin Receptor S1P Receptor Cannabinoid Receptor Hedgehog/Smoothened SGLT Opioid Receptor GPR CCR MT Receptor LPA Receptor PAFR OX Receptor PKA cAMP Vasopressin Receptor Protease-activated Receptor Adenosine Receptor Glucagon Receptor TAAR GRK AdipoR Prostaglandin Receptor CCK receptor GHSR Guanylate Cyclase GPCR19 GPR139 NPY receptor PAR TAS1R Sigma Receptor RGS Imidazoline Receptor Angiotensin Receptor PKG Neurokinin Receptor FPR DOCK Taste Receptor Melanocortin Receptor Somatostatin Receptor Bombesin Receptor Bradykinin Receptor CRFR GNRH Receptor TSH Receptor Parathyroid Hormone Receptor GLP-1 Receptor Adenylyl Cyclase Apelin receptor Arrestin GTPase MCHR Orphan Receptor Oxytocin Receptor Platelet aggregation RXFP receptor

All (19)
P-gp Inhibitors (13)
P-gp Agonist (1)
P-gp Modulators (4)
New P-gp Products

Cat.No.	Product Name	Information	Product Use Citations
S8028	Tariquidar	Tariquidar is a potent and selective noncompetitive inhibitor of P-glycoprotein with K_d 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
S1481	Zosuquidar 3HCl	Zosuquidar 3HCl is a potent modulator of P-glycoprotein-mediated multi-drug resistance with K_i 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
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
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.
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 Front Pharmacol, 2025, 16:1530270
S8130^New	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.
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.
S9201	Levistilide A	Levistilide A (Diligustilide), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is a potential P-gp modulator and used for treating cancer.
S9563	Evodine	Evodine, a natural product extracted from Evodiae fructus (EF), is a biomarker for quality assessment of EF in the Chinese Pharmacopoeia. This compound is a potent P-gp inhibitor.
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.
S4202	Verapamil HCl	Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.	Cancer Cell, 2025, 43(4):776-796.e14 Nat Commun, 2025, 16(1):7115 Blood Sci, 2025, 7(2):e00236
S7124	SC144	SC144 is the first-in-class orally active small-molecule gp130 inhibitor that induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes.	Cell Rep Med, 2025, S2666-3791(25)00102-8 Respir Res, 2025, 26(1):285 bioRxiv, 2025, 2025.01.20.633954
S4662	Atazanavir	Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. This compound is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.	Int J Mol Sci, 2022, 23(23)15380 Chemistry, 2022, e202202798. Cells, 2021, 10(12)3458
S3600	Schisandrin B	Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety.	Phytomedicine, 2025, 141:156672 Front Pharmacol, 2025, 16:1547685 Sci Rep, 2025, 15(1):8452
E4980	Verapamil	Verapamil(Iproveratril,Dilacoran), is a phenylalkylamine derivative which is an antagonist of calcium influx and also an inhibitor P-gp and CYP3A4. It exhibits potency in treatment for angina, cardiac arrhythmias, cardiomyopathies and hypertension.	Nat Commun, 2025, 16(1):8069 J Am Heart Assoc, 2025, 14(1):e037400 Pharmaceuticals (Basel), 2025, 18(2)181
S8028	Tariquidar	Tariquidar is a potent and selective noncompetitive inhibitor of P-glycoprotein with K_d 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
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
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).
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 Front Pharmacol, 2025, 16:1530270
S9563	Evodine	Evodine, a natural product extracted from Evodiae fructus (EF), is a biomarker for quality assessment of EF in the Chinese Pharmacopoeia. This compound is a potent P-gp inhibitor.
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.
S4202	Verapamil HCl	Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.	Cancer Cell, 2025, 43(4):776-796.e14 Nat Commun, 2025, 16(1):7115 Blood Sci, 2025, 7(2):e00236
S7124	SC144	SC144 is the first-in-class orally active small-molecule gp130 inhibitor that induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes.	Cell Rep Med, 2025, S2666-3791(25)00102-8 Respir Res, 2025, 26(1):285 bioRxiv, 2025, 2025.01.20.633954
S3600	Schisandrin B	Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety.	Phytomedicine, 2025, 141:156672 Front Pharmacol, 2025, 16:1547685 Sci Rep, 2025, 15(1):8452
E4980	Verapamil	Verapamil(Iproveratril,Dilacoran), is a phenylalkylamine derivative which is an antagonist of calcium influx and also an inhibitor P-gp and CYP3A4. It exhibits potency in treatment for angina, cardiac arrhythmias, cardiomyopathies and hypertension.	Nat Commun, 2025, 16(1):8069 J Am Heart Assoc, 2025, 14(1):e037400 Pharmaceuticals (Basel), 2025, 18(2)181
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.
S1481	Zosuquidar 3HCl	Zosuquidar 3HCl is a potent modulator of P-glycoprotein-mediated multi-drug resistance with K_i 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
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.
S9201	Levistilide A	Levistilide A (Diligustilide), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is a potential P-gp modulator and used for treating cancer.
S4662	Atazanavir	Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. This compound is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.	Int J Mol Sci, 2022, 23(23)15380 Chemistry, 2022, e202202798. Cells, 2021, 10(12)3458
S8130^New	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.

P-gp

Transmembrane Transporters

Signaling Pathway Map