| E0080 |
UCLA GP130 2
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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.
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| S9201 |
Levistilide A
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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.
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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 non-toxic 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 tumours.
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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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| S4662 |
Atazanavir
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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.
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Int J Mol Sci, 2022, 23(23)15380
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Chemistry, 2022, e202202798.
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Cells, 2021, 10(12)3458
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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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