S8028 |
Tariquidar
|
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. |
-
Drug Resist Updat, 2024, 73:101066
-
Int J Mol Sci, 2024, 25(6)3107
-
Exp Hematol, 2024, S0301-472X(24)00516-2
|
|
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. |
-
Hepatol Commun, 2024, 8(5)e0437
-
Adv Healthc Mater, 2022, e2201984
-
Mol Cancer Ther, 2022, 21 (7): 1227–1235.
|
|
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. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
NPJ Precis Oncol, 2024, 8(1):94
-
Int J Mol Sci, 2024, 25(18)10162
|
|
S7772 |
Elacridar (GF120918)
|
Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.
|
-
Cell Death Dis, 2024, 15(8):558
-
Oncogene, 2024, 43(26):2038-2050
-
Pharmaceutics, 2024, 16(10)1290
|
|
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. |
-
Nat Med, 2024, 10.1038/s41591-024-02953-4
-
Nat Commun, 2024, 15(1):1041
-
Cell Stem Cell, 2023, 30(10):1382-1391.e5
|
|
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. Atazanavir 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
|
|
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. Sinapine 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). |
|
|
E1781New |
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. |
|
|
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. |
-
Drug Des Devel Ther, 2024, 18:4241-4256
-
Viruses, 2022, 14(2)353
-
Pharmacol Res, 2021, 166:105459
|
|
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. |
|
|
E4980New |
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. |
-
Cell Death Dis, 2024, 15(11):855
|
|
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. Evodine is a potent P-gp inhibitor. |
|
|
E1742New |
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. |
|
|
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. |
|
|
S8028 |
Tariquidar
|
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. |
- Drug Resist Updat, 2024, 73:101066
- Int J Mol Sci, 2024, 25(6)3107
- Exp Hematol, 2024, S0301-472X(24)00516-2
|
|
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. |
- J Immunother Cancer, 2024, 12(11)e009805
- NPJ Precis Oncol, 2024, 8(1):94
- Int J Mol Sci, 2024, 25(18)10162
|
|
S7772 |
Elacridar (GF120918)
|
Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.
|
- Cell Death Dis, 2024, 15(8):558
- Oncogene, 2024, 43(26):2038-2050
- Pharmaceutics, 2024, 16(10)1290
|
|
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. |
- Nat Med, 2024, 10.1038/s41591-024-02953-4
- Nat Commun, 2024, 15(1):1041
- Cell Stem Cell, 2023, 30(10):1382-1391.e5
|
|
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. Sinapine 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). |
|
|
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. |
- Drug Des Devel Ther, 2024, 18:4241-4256
- Viruses, 2022, 14(2)353
- Pharmacol Res, 2021, 166:105459
|
|
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. |
|
|
E4980New |
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. |
- Cell Death Dis, 2024, 15(11):855
|
|
S9563 |
Evodine
|
Evodine, a natural product extracted from Evodiae fructus (EF), is a biomarker for quality assessment of EF in the Chinese Pharmacopoeia. Evodine is a potent P-gp inhibitor. |
|
|
E1742New |
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. |
|
|
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. |
- Hepatol Commun, 2024, 8(5)e0437
- Adv Healthc Mater, 2022, e2201984
- Mol Cancer Ther, 2022, 21 (7): 1227–1235.
|
|
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. Atazanavir 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
|
|
E1781New |
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. |
|
|