| S8028 |
Tariquidar (XR9576)
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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.
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Nat Commun, 2025, 16(1):5511
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J Transl Med, 2025, 23(1):542
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Cells, 2025, 14(16)1276
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| S7772 |
Elacridar (GF120918)
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Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.
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Nat Commun, 2025, 16(1):5511
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Cell Rep Med, 2025, 6(6):102160
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Nanoscale, 2025, 17(16):9947-9962
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| S4746 |
(20S)-Protopanaxadiol
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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.
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Front Pharmacol, 2025, 16:1530270
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| S9145 |
Solamargine
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Solamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition.
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Sci Rep, 2016, 6:36721
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| S3235 |
Sinapine
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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.
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Gene, 2022, 827:146460
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| S0921 |
Wilforine
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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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| S3431 |
Encequidar (HM30181)
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Encequidar (HM30181, HM30181A) is a potent and selective inhibitor of the adenosine triphosphate-binding cassette transporter P-glycoprotein (P-gp).
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| S9563 |
Evodine
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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.
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| E1742 |
Reversan
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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.
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| S4202 |
Verapamil HCl
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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.
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Cancer Cell, 2025, 43(4):776-796.e14
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Nat Commun, 2025, 16(1):7115
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Blood Sci, 2025, 7(2):e00236
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| S7124 |
SC144
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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.
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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Respir Res, 2025, 26(1):285
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bioRxiv, 2025, 2025.01.20.633954
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| S3600 |
Schisandrin B
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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.
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Phytomedicine, 2025, 141:156672
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Front Pharmacol, 2025, 16:1547685
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Sci Rep, 2025, 15(1):8452
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| E4980 |
Verapamil
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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.
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Nat Commun, 2025, 16(1):8069
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J Am Heart Assoc, 2025, 14(1):e037400
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Pharmaceuticals (Basel), 2025, 18(2)181
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