P-gp

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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(2) 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 Med Chem, 2016, 59(13):6353-69 Cell Chem Biol, 2018, 25(2):135-142	Mutations of the polar residues Y307, Q725 and Y953 to alanine, cysteine and phenylalanine (Y953F only) were tested for their effect on the modulation of basal ATPase activity of P-gp by drugs. Basal activity of cysless WT and mutant P-gps was taken as zero, inhibition was calculated as percentage of the basal activity and shown with downward bars (negative values), while stimulation was calculated as percentage of the basal activity and shown with upward bars (positive values). Bars are colored black for cysless WT or triple A (Y307A/Q725A/Y953A) while they are grey for the single mutants (Y307A/C, Q725A/C, Y953A/C/F). At least three experiments were carried out with duplicate samples for each mutant with indicated compounds, and errors bars denote the standard deviations.
S7772	Elacridar (GF120918) Elacridar (GF120918)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。	J Exp Clin Cancer Res, 2017, 36(1):122 Arch Toxicol, 2018, 92(6):2027-2042 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。	Cell Death Dis, 2016, 7(8):e2339 J Exp Clin Cancer Res, 2018, 37(1):186	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。	Pharmacol Res, 2013, 67(1):79-83 Mol Pharm, 2016, 13(2):512-9 J Lipid Res, 2014, 56(1):60-9	Effect of P-gp expression on cell survival and proliferation of DNR and Zosuquidar(ZSQ) treated cells.
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 J Med Chem,2016, 59(13):6353-69 Cell Chem Biol,2018, 25(2):135-142	Mutations of the polar residues Y307, Q725 and Y953 to alanine, cysteine and phenylalanine (Y953F only) were tested for their effect on the modulation of basal ATPase activity of P-gp by drugs. Basal activity of cysless WT and mutant P-gps was taken as zero, inhibition was calculated as percentage of the basal activity and shown with downward bars (negative values), while stimulation was calculated as percentage of the basal activity and shown with upward bars (positive values). Bars are colored black for cysless WT or triple A (Y307A/Q725A/Y953A) while they are grey for the single mutants (Y307A/C, Q725A/C, Y953A/C/F). At least three experiments were carried out with duplicate samples for each mutant with indicated compounds, and errors bars denote the standard deviations.
S7772	Elacridar (GF120918) Elacridar (GF120918)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。	J Exp Clin Cancer Res,2017, 36(1):122 Arch Toxicol,2018, 92(6):2027-2042 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。	Cell Death Dis,2016, 7(8):e2339 J Exp Clin Cancer Res,2018, 37(1):186	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。	Pharmacol Res, 2013, 67(1):79-83 Mol Pharm, 2016, 13(2):512-9 J Lipid Res, 2014, 56(1):60-9	Effect of P-gp expression on cell survival and proliferation of DNR and Zosuquidar(ZSQ) treated cells.
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。

Pharmacol Res, 2013, 67(1):79-83

Mol Pharm, 2016, 13(2):512-9

J Lipid Res, 2014, 56(1):60-9

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