P-gp

信号通路图

研究领域

抑制剂选择性比较

P-gp产品

所有产品 P-gp抑制剂(5) P-gp调节剂(3) 新P-gp产品

产品目录	产品描述	文献引用	实验数据
S8028	Tariquidar Tariquidar是一种有效的，选择性的，非竞争性P-glycoprotein抑制剂，在CHrB30细胞系中K_d为5.1 nM，作用于MDR细胞系逆转耐药性。Phase 3。	Cancer Res, 2019, 10.1158/0008-5472.CAN-18-1888 J Control Release, 2019, 317:67-77 Breast Cancer Res, 2019, 21(1):7	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)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。	Arch Toxicol, 2018, 92(6):2027-2042 J Exp Clin Cancer Res, 2017, 36(1):122 Biochem Pharmacol, 2016, 101:40-53	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 (Sch B)是中草药五味子(Turcz.)中含量最丰富的二苯并环辛二烯木酚素。它是一种安全的ATR和P-gp抑制剂。	Inflammation, 2017, 40(6):1903-1911
S7124	SC144 SC144是一种具有口服活性的小分子gp130抑制剂，能够诱导gp130(S782)磷酸化和去糖基化、抑制STAT3磷酸化和核转位，并进一步抑制其下游靶基因的表达。	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.
S1481	Zosuquidar (LY335979) 3HCl Zosuquidar (LY335979) 3HCl是一种有效的P-glycoprotein介导的多药耐抗性的调节剂，无细胞试验中K_i为60 nM。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^New	RCGD423 RCGD-423是gp130信号调节剂，可调节软骨生长和分化。
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.

产品目录	产品描述	文献引用	实验数据
S8028	Tariquidar Tariquidar是一种有效的，选择性的，非竞争性P-glycoprotein抑制剂，在CHrB30细胞系中K_d为5.1 nM，作用于MDR细胞系逆转耐药性。Phase 3。	Cancer Res,2019, 10.1158/0008-5472.CAN-18-1888 J Control Release,2019, 317:67-77 Breast Cancer Res,2019, 21(1):7	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)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。	Arch Toxicol,2018, 92(6):2027-2042 J Exp Clin Cancer Res,2017, 36(1):122 Biochem Pharmacol,2016, 101:40-53	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 (Sch B)是中草药五味子(Turcz.)中含量最丰富的二苯并环辛二烯木酚素。它是一种安全的ATR和P-gp抑制剂。	Inflammation,2017, 40(6):1903-1911
S7124	SC144 SC144是一种具有口服活性的小分子gp130抑制剂，能够诱导gp130(S782)磷酸化和去糖基化、抑制STAT3磷酸化和核转位，并进一步抑制其下游靶基因的表达。	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.

产品目录	产品描述	文献引用	实验数据
S1481	Zosuquidar (LY335979) 3HCl Zosuquidar (LY335979) 3HCl是一种有效的P-glycoprotein介导的多药耐抗性的调节剂，无细胞试验中K_i为60 nM。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^New	RCGD423 RCGD-423是gp130信号调节剂，可调节软骨生长和分化。
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.

产品目录

产品描述

文献引用

实验数据

S1481

Zosuquidar (LY335979) 3HCl

Zosuquidar (LY335979) 3HCl是一种有效的P-glycoprotein介导的多药耐抗性的调节剂，无细胞试验中K_i为60 nM。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^New

RCGD423

RCGD-423是gp130信号调节剂，可调节软骨生长和分化。

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.

研究领域

产品类型

P-gp

信号通路图

研究领域

抑制剂选择性比较

P-gp产品