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decynium22  (MedChemExpress)
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MedChemExpress decynium22
Inhibition of organic cation transporters by TKIs. (A) The protein sequence of hOCT1, hOCT2, and hOCT3 was aligned by a multiple sequence alignment program (MAFFT). (B) OCT1 protein sequence from indicated organisms was aligned by a multiple sequence alignment program (MAFFT). (C) HEK293 cells were transiently transfected with wild-type (WT), Y240F, Y361F, and Y376F mutant plasmids, uptake assays were performed using [ 14 C] TEA (2 µM) for 15 min. Cellular accumulation of [ 14 C] TEA was determined by liquid scintillation counter, and the graph represents relative uptake values compared to wild-type after normalization of protein levels. (D) Relative transporter function in HEK293 cells stably transfected with hOCT1 was evaluated by a substrate drug TEA in the presence of FDA-approved TKIs (10 µM) previously found to inhibit OCT2. Lapatinib was included as a negative-control TKI, and <t>decynium22</t> as a non-TKI positive control inhibitor. The graph represents relative transport activity of indicated substrate drug compared to DMSO. * p < 0.05 vs. wild-type control. All values represent mean ± SEM.
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Inhibition of organic cation transporters by TKIs. (A) The protein sequence of hOCT1, hOCT2, and hOCT3 was aligned by a multiple sequence alignment program (MAFFT). (B) OCT1 protein sequence from indicated organisms was aligned by a multiple sequence alignment program (MAFFT). (C) HEK293 cells were transiently transfected with wild-type (WT), Y240F, Y361F, and Y376F mutant plasmids, uptake assays were performed using [ 14 C] TEA (2 µM) for 15 min. Cellular accumulation of [ 14 C] TEA was determined by liquid scintillation counter, and the graph represents relative uptake values compared to wild-type after normalization of protein levels. (D) Relative transporter function in HEK293 cells stably transfected with hOCT1 was evaluated by a substrate drug TEA in the presence of FDA-approved TKIs (10 µM) previously found to inhibit OCT2. Lapatinib was included as a negative-control TKI, and decynium22 as a non-TKI positive control inhibitor. The graph represents relative transport activity of indicated substrate drug compared to DMSO. * p < 0.05 vs. wild-type control. All values represent mean ± SEM.

Journal: Frontiers in Pharmacology

Article Title: Influence of YES1 Kinase and Tyrosine Phosphorylation on the Activity of OCT1

doi: 10.3389/fphar.2021.644342

Figure Lengend Snippet: Inhibition of organic cation transporters by TKIs. (A) The protein sequence of hOCT1, hOCT2, and hOCT3 was aligned by a multiple sequence alignment program (MAFFT). (B) OCT1 protein sequence from indicated organisms was aligned by a multiple sequence alignment program (MAFFT). (C) HEK293 cells were transiently transfected with wild-type (WT), Y240F, Y361F, and Y376F mutant plasmids, uptake assays were performed using [ 14 C] TEA (2 µM) for 15 min. Cellular accumulation of [ 14 C] TEA was determined by liquid scintillation counter, and the graph represents relative uptake values compared to wild-type after normalization of protein levels. (D) Relative transporter function in HEK293 cells stably transfected with hOCT1 was evaluated by a substrate drug TEA in the presence of FDA-approved TKIs (10 µM) previously found to inhibit OCT2. Lapatinib was included as a negative-control TKI, and decynium22 as a non-TKI positive control inhibitor. The graph represents relative transport activity of indicated substrate drug compared to DMSO. * p < 0.05 vs. wild-type control. All values represent mean ± SEM.

Article Snippet: Reference standards of decynium22, a positive control inhibitor, as well as the TKIs bosutinib, dasatinib, gilteritinib, ibrutinib, lapatinib, sunitinib, vandetanib, and CH6953755 were obtained from MedChemExpress (Monmouth Junction, NJ).

Techniques: Inhibition, Sequencing, Transfection, Mutagenesis, Stable Transfection, Negative Control, Positive Control, Activity Assay, Control