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)
カタログ番号	製品カタログ	水	DMSO	アルコール
S8028	Tariquidar	<1 mg/mL	52 mg/mL	<1 mg/mL
S7772	Elacridar (GF120918)	<1 mg/mL	8 mg/mL	<1 mg/mL
S3600	Schisandrin B (Sch B)	<1 mg/mL	80 mg/mL	10 mg/mL
S7124	SC144	<1 mg/mL	28 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
S6579	RCGD423	<1 mg/mL	66 mg/mL	32 mg/mL
S9201	Levistilide A	-1 mg/mL	76 mg/mL	-1 mg/mL

P-gp製品

All (8) P-gp阻害剤(5) P-gpモジュレータ(3) 新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	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.	J Clin Invest, 2019, 129(10):4377-4392 Cancer Res, 2019, 10.1158/0008-5472.CAN-18-1888 J Control Release, 2019, 317:67-77	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, each with assays in triplicate); Asc: ascorbic acid, Zq: zosuquidar, Tq: tariquidar.
S7772	Elacridar (GF120918) Elacridar (GF120918) is a potent P-gp (MDR-1) and BCRP inhibitor.	Nat Commun, 2019, 10(1):1295 Biochim Biophys Acta Mol Basis Dis, 2019, 10.1016/j.bbadis.2019.165625 Cell Death Dis, 2018, 9(8):810	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.
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.	Inflammation, 2017, 40(6):1903-1911
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.	J Exp Clin Cancer Res, 2018, 37(1):186 J Lipid Res, 2017, 58(11):2102-2113 Cell Death Dis, 2016, 7(8):e2339	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.
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
S1481	Zosuquidar (LY335979) 3HCl Zosuquidar (LY335979) 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.	J Lipid Res, 2019, 60(6):1078-1086 Toxicol In Vitro, 2019, 54:33-40 Biochem Biophys Res Commun, 2019, 514(4):1154-1159	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.
S6579^新	RCGD423 RCGD-423 is a modulator of gp130 signalling that regulates cartilage growth and differentiation.
S9201	Levistilide A Levistilide A, a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is a potential P-gp modulator and used for treating cancer.

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	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.	J Clin Invest, 2019, 129(10):4377-4392 Cancer Res, 2019, 10.1158/0008-5472.CAN-18-1888 J Control Release, 2019, 317:67-77	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, each with assays in triplicate); Asc: ascorbic acid, Zq: zosuquidar, Tq: tariquidar.
S7772	Elacridar (GF120918) Elacridar (GF120918) is a potent P-gp (MDR-1) and BCRP inhibitor.	Nat Commun, 2019, 10(1):1295 Biochim Biophys Acta Mol Basis Dis, 2019, 10.1016/j.bbadis.2019.165625 Cell Death Dis, 2018, 9(8):810	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.
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.	Inflammation, 2017, 40(6):1903-1911
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.	J Exp Clin Cancer Res, 2018, 37(1):186 J Lipid Res, 2017, 58(11):2102-2113 Cell Death Dis, 2016, 7(8):e2339	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.
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

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) 3HCl Zosuquidar (LY335979) 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.	J Lipid Res, 2019, 60(6):1078-1086 Toxicol In Vitro, 2019, 54:33-40 Biochem Biophys Res Commun, 2019, 514(4):1154-1159	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.
S6579^新	RCGD423 RCGD-423 is a modulator of gp130 signalling that regulates cartilage growth and differentiation.
S9201	Levistilide A Levistilide A, a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is a potential P-gp modulator and used for treating cancer.

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) 3HCl

Zosuquidar (LY335979) 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.

J Lipid Res, 2019, 60(6):1078-1086

Toxicol In Vitro, 2019, 54:33-40

Biochem Biophys Res Commun, 2019, 514(4):1154-1159

S6579^新

RCGD423

RCGD-423 is a modulator of gp130 signalling that regulates cartilage growth and differentiation.

S9201

Levistilide A

Levistilide A, a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is a potential P-gp modulator and used for treating cancer.

研究分野別

製品類型

P-gp

シグナル伝達経路

研究分野

阻害剤の選択性比較