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 Breast Cancer Res, 2019, 21(1):7 Cell Chem Biol, 2018, 25(2):135-142	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
S9145^New	Solamargine Solamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition.
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.
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^New	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 Breast Cancer Res,2019, 21(1):7 Cell Chem Biol,2018, 25(2):135-142	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
S9145^New	Solamargine Solamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition.
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.

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^New	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^New

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