|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|
|S9145||Solamargine||-1 mg/mL||100 mg/mL||-1 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 is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM in CHrB30 cell line, reverses drug resistance in MDR cell Lines. 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) is a potent P-gp (MDR-1) and BCRP inhibitor.
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.
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.
Solamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition.
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.
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 is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM in a cell-free assay. 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.