P-gp
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S8028 | Tariquidar | <1 mg/mL | 52 mg/mL | <1 mg/mL |
| S4202 | Verapamil HCl | 50 mg/mL | 98 mg/mL | 12 mg/mL |
| S0921 | Wilforine | <1 mg/mL | 100 mg/mL | ''<1 mg/mL |
| S7772 | Elacridar (GF120918) | <1 mg/mL | 8 mg/mL | '<1 mg/mL |
| S3235 | Sinapine | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S3600 | Schisandrin B (Sch B) | <1 mg/mL | 80 mg/mL | 10 mg/mL |
| S4746 | (20S)-Protopanaxadiol | <1 mg/mL | 92 mg/mL | 33 mg/mL |
| S7124 | SC144 | <1 mg/mL | 28 mg/mL | <1 mg/mL |
| S9563 | Evodine | -1 mg/mL | 66 mg/mL | -1 mg/mL |
| S9145 | Solamargine | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S1481 | Zosuquidar (LY335979) 3HCl | 23 mg/mL | 100 mg/mL | <1 mg/mL |
| S9201 | Levistilide A | -1 mg/mL | 76 mg/mL | -1 mg/mL |
| S4662 | Atazanavir | <1 mg/mL | 71 mg/mL | 32 mg/mL |
P-gp製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S8028 |
TariquidarTariquidar (XR9576) 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. |
Effects of LEV alone, or in combination with MDRIs, on the migration of L3 stage H. contortus Kirby (A) and WAL (B) larvae; LEV alone shown with solid lines and closed symbols, IVM plus MDRIs shown as dashed lines and open symbols. The concentration of each MDRI in g/mL is shown as subscript after the MDRI name. Each data point represents mean ± SE, n = 9 (pooled data from three experiments, |
|
| S4202 |
Verapamil HClVerapamil 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. |
The proportion of SP cells in HepG2 and HCCLM3 cell lines were 0.16% and 32.2%, which reduced to 0% and 0.28% in the presence of verapamil.
|
|
| S0921新 |
WilforineWilforine (WR), a sesquiterpene pyridine alkaloid found in T. wilfordii plants, significantly inhibits the efflux activity of P-glycoprotein (P-gp). |
||
| S7772 |
Elacridar (GF120918)Elacridar (GF120918, GW120918) is a potent P-gp (MDR-1) and BCRP inhibitor. |
Impact of 10 μM elacridar on the intracellular accumulation of 10 μM nintedanib in DMS114 and DMS114/NIN cells was analyzed by confocal fluorescence microscopy after 1 h drug exposure. The scale bar indicates 10 μm.
|
|
| S3235新 |
SinapineSinapine 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. |
||
| S3600 |
Schisandrin B (Sch 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. |
||
| S4746 |
(20S)-Protopanaxadiol20(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. |
||
| S7124 |
SC144SC144 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. |
Suppression of gp130/STAT3 blocks the protective effect of SPRC against Dox-induced cell apoptosis. Cardiomyocytes were pretreated with/without SC144 before SPRC incubation, followed by Dox (1 μM) stimulation for 24 h. (a) Morphological apoptosis was determined by Hoechst 33258 staining. Scale bars, 50 μm.
|
|
| S9563 |
EvodineEvodine, 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. |
||
| S9145 |
SolamargineSolamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition. |
||
| S1481 |
Zosuquidar (LY335979) 3HClZosuquidar 3HCl (LY335979, RS 33295-198, D06387) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM in a cell-free assay. Phase 3. |
Inhibition of doxorubicin compartmentalization by combined treatment with inhibitors of Abcb1 and Abcc1. A: The cells had been incubated with vehicle or 1 uM zosuquidar plus 15 uM MK571 (ZO/MK), before addition of 1 uM doxorubicin (Doxo) and further cultivation in serum-free medium for 16 h. Shown are typical images of doxorubicin (red) and Hoechst 33342 (blue) fluorescence in Sgpl1+/+ - and Sgpl1-/- -MEFs after treatment as indicated. Two images of Sgpl1-/- -cells treated with doxorubicin plus ZO/MK were selected to show the range of the cellular response. B: Hoechst 33342 staining in MEFs that had been incubated with ZO/MK in the absence of doxorubicin.
|
|
| S9201 |
Levistilide ALevistilide 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 |
AtazanavirAtazanavir (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. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S8028 |
TariquidarTariquidar (XR9576) 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. |
Effects of LEV alone, or in combination with MDRIs, on the migration of L3 stage H. contortus Kirby (A) and WAL (B) larvae; LEV alone shown with solid lines and closed symbols, IVM plus MDRIs shown as dashed lines and open symbols. The concentration of each MDRI in g/mL is shown as subscript after the MDRI name. Each data point represents mean ± SE, n = 9 (pooled data from three experiments, |
|
| S4202 |
Verapamil HClVerapamil 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. |
The proportion of SP cells in HepG2 and HCCLM3 cell lines were 0.16% and 32.2%, which reduced to 0% and 0.28% in the presence of verapamil.
|
|
| S0921新 |
WilforineWilforine (WR), a sesquiterpene pyridine alkaloid found in T. wilfordii plants, significantly inhibits the efflux activity of P-glycoprotein (P-gp). |
||
| S7772 |
Elacridar (GF120918)Elacridar (GF120918, GW120918) is a potent P-gp (MDR-1) and BCRP inhibitor. |
Impact of 10 μM elacridar on the intracellular accumulation of 10 μM nintedanib in DMS114 and DMS114/NIN cells was analyzed by confocal fluorescence microscopy after 1 h drug exposure. The scale bar indicates 10 μm.
|
|
| S3235新 |
SinapineSinapine 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. |
||
| S3600 |
Schisandrin B (Sch 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. |
||
| S4746 |
(20S)-Protopanaxadiol20(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. |
||
| S7124 |
SC144SC144 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. |
Suppression of gp130/STAT3 blocks the protective effect of SPRC against Dox-induced cell apoptosis. Cardiomyocytes were pretreated with/without SC144 before SPRC incubation, followed by Dox (1 μM) stimulation for 24 h. (a) Morphological apoptosis was determined by Hoechst 33258 staining. Scale bars, 50 μm.
|
|
| S9563 |
EvodineEvodine, 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. |
||
| S9145 |
SolamargineSolamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1481 |
Zosuquidar (LY335979) 3HClZosuquidar 3HCl (LY335979, RS 33295-198, D06387) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM in a cell-free assay. Phase 3. |
2020, 2;12(3) pii: E577 2020, S0006-2952(20)30604-3 2020, 12;14:1799-1811 |
Inhibition of doxorubicin compartmentalization by combined treatment with inhibitors of Abcb1 and Abcc1. A: The cells had been incubated with vehicle or 1 uM zosuquidar plus 15 uM MK571 (ZO/MK), before addition of 1 uM doxorubicin (Doxo) and further cultivation in serum-free medium for 16 h. Shown are typical images of doxorubicin (red) and Hoechst 33342 (blue) fluorescence in Sgpl1+/+ - and Sgpl1-/- -MEFs after treatment as indicated. Two images of Sgpl1-/- -cells treated with doxorubicin plus ZO/MK were selected to show the range of the cellular response. B: Hoechst 33342 staining in MEFs that had been incubated with ZO/MK in the absence of doxorubicin.
|
| S9201 |
Levistilide ALevistilide 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 |
AtazanavirAtazanavir (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. |
2020, 10.1021/acsinfecdis.0c00536 2020, 48(12):1264-1270 2020, AAC.00872-20 |
