|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|
|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|
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Kd为5.1 nM，作用于MDR细胞系逆转耐药性。Phase 3。
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.
Elacridar (GF120918)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。
Effect of drugs on the photo-crosslinking of cysless WT and triple A (Y307A/Q725A/Y953A) mutant P-gp with IAAP. Crude membranes expressing cysless WT or mutant P-gp (60-80 μg protein) were treated with the indicated concentrations of drug in 100 μL buffer containing 50 mM MES-Tris pH 6.8 for 10 min at 37 °C. Samples were then photo-crosslinked with 4–6 nM IAAP at 4 °C as described in Section 2. IAAP-labeling of the cysless WT and Triple A mutant P-gp with no addition of drug was taken as 100% labeling. Both panels show a representative autoradiogram (at the top) and the quantification of the IAAP-labeling (at the bottom). Lane 1, control (DMSO solvent); 2, 1 μM zosuquidar; 3, 1 μM elacridar; and 4, 1 μM tariquidar. Data represent the mean ± the standard deviations for n = 3. Left panel, cysless WT; right panel, Triple A (Y307A/Q725A/Y953A) mutant.
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。
Solamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition.
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.
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Ki为60 nM。Phase 3。
Effect of P-gp expression on cell survival and proliferation of DNR and Zosuquidar(ZSQ) treated cells.
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.