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Influence of KSQ‐4279 on AKT and ERK transduction and analysis of KSQ‐4279 binding with ABCB1/ABCG2/ABCC1. ( A ) Western blot showed the action of KSQ‐4279 on AKT and ERK transduction. GAPDH was as an input control. ( B ) Bar graphs for the relative protein expression of the various signaling molecules detected in (A). Data were reported as mean ± SD (* p < 0.05; ** p < 0.01; *** p < 0.001). ( C ) Binding of KSQ‐4279 with ABCB1, ABCG2, and ABCC1 were assessed by CETSAs. Aliquots of cell lysates incubated with DMSO or KSQ‐4279 (10 µM) were heated at indicated temperatures, and the presence of KSQ‐4279‐bound ABCB1/ABCG2/ABCC1 proteins was analyzed via western blots. ( D ) Molecular docking of (a and b) KSQ‐4279, (c) paclitaxel, and (d) vincristine with to substrate‐binding region of ABCB1. ( E ) Molecular docking of (a and b) KSQ‐4279, (c) mitoxantrone, and (d) <t>topotecan</t> to the substrate‐binding area of ABCG2. ( F ) Molecular docking of (a and b) KSQ‐4279, and (c) doxorubicin to the substrate‐binding domain of ABCC1. Molecular 3D structures were obtained from the web of PubChem ( https://pubchem.ncbi.nlm.nih.gov/ ), and the crystal structures of ABC transporters were obtained from the web of Protein Data Bank ( https://www.rcsb.org/ ). The docking was performed by using software of AutoDock Vina.
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https://www.bioz.com/result/topotecan/product/MedChemExpress
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topotecan hydrochloride  (Molcan Corporation)
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Reporter fluorescence changes in response to topoisomerase inhibitors. Flow cytometry histograms comparing green fluorescence intensities in 17-week-old reporter organoids exposed to A) 1 µM <t>topotecan,</t> B) 1 µM irinotecan, and C) 0.2% DMSO in water (vehicle control). The parental and reporter iPSCs were used to determine the GF +/-gate. a.u. - arbitrary units.
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Reporter fluorescence changes in response to topoisomerase inhibitors. Flow cytometry histograms comparing green fluorescence intensities in 17-week-old reporter organoids exposed to A) 1 µM <t>topotecan,</t> B) 1 µM irinotecan, and C) 0.2% DMSO in water (vehicle control). The parental and reporter iPSCs were used to determine the GF +/-gate. a.u. - arbitrary units.
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topotecan  (Glaxo Smith)
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Reporter fluorescence changes in response to topoisomerase inhibitors. Flow cytometry histograms comparing green fluorescence intensities in 17-week-old reporter organoids exposed to A) 1 µM <t>topotecan,</t> B) 1 µM irinotecan, and C) 0.2% DMSO in water (vehicle control). The parental and reporter iPSCs were used to determine the GF +/-gate. a.u. - arbitrary units.
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Influence of KSQ‐4279 on AKT and ERK transduction and analysis of KSQ‐4279 binding with ABCB1/ABCG2/ABCC1. ( A ) Western blot showed the action of KSQ‐4279 on AKT and ERK transduction. GAPDH was as an input control. ( B ) Bar graphs for the relative protein expression of the various signaling molecules detected in (A). Data were reported as mean ± SD (* p < 0.05; ** p < 0.01; *** p < 0.001). ( C ) Binding of KSQ‐4279 with ABCB1, ABCG2, and ABCC1 were assessed by CETSAs. Aliquots of cell lysates incubated with DMSO or KSQ‐4279 (10 µM) were heated at indicated temperatures, and the presence of KSQ‐4279‐bound ABCB1/ABCG2/ABCC1 proteins was analyzed via western blots. ( D ) Molecular docking of (a and b) KSQ‐4279, (c) paclitaxel, and (d) vincristine with to substrate‐binding region of ABCB1. ( E ) Molecular docking of (a and b) KSQ‐4279, (c) mitoxantrone, and (d) topotecan to the substrate‐binding area of ABCG2. ( F ) Molecular docking of (a and b) KSQ‐4279, and (c) doxorubicin to the substrate‐binding domain of ABCC1. Molecular 3D structures were obtained from the web of PubChem ( https://pubchem.ncbi.nlm.nih.gov/ ), and the crystal structures of ABC transporters were obtained from the web of Protein Data Bank ( https://www.rcsb.org/ ). The docking was performed by using software of AutoDock Vina.

Journal: MedComm

Article Title: KSQ‐4279, an Inhibitor of Ubiquitin Specific Peptidase 1, Enhanced the Chemotherapeutic Efficacy in ABCB1/ABCG2/ABCC1‐Mediated Multidrug Resistant Cancers

doi: 10.1002/mco2.70517

Figure Lengend Snippet: Influence of KSQ‐4279 on AKT and ERK transduction and analysis of KSQ‐4279 binding with ABCB1/ABCG2/ABCC1. ( A ) Western blot showed the action of KSQ‐4279 on AKT and ERK transduction. GAPDH was as an input control. ( B ) Bar graphs for the relative protein expression of the various signaling molecules detected in (A). Data were reported as mean ± SD (* p < 0.05; ** p < 0.01; *** p < 0.001). ( C ) Binding of KSQ‐4279 with ABCB1, ABCG2, and ABCC1 were assessed by CETSAs. Aliquots of cell lysates incubated with DMSO or KSQ‐4279 (10 µM) were heated at indicated temperatures, and the presence of KSQ‐4279‐bound ABCB1/ABCG2/ABCC1 proteins was analyzed via western blots. ( D ) Molecular docking of (a and b) KSQ‐4279, (c) paclitaxel, and (d) vincristine with to substrate‐binding region of ABCB1. ( E ) Molecular docking of (a and b) KSQ‐4279, (c) mitoxantrone, and (d) topotecan to the substrate‐binding area of ABCG2. ( F ) Molecular docking of (a and b) KSQ‐4279, and (c) doxorubicin to the substrate‐binding domain of ABCC1. Molecular 3D structures were obtained from the web of PubChem ( https://pubchem.ncbi.nlm.nih.gov/ ), and the crystal structures of ABC transporters were obtained from the web of Protein Data Bank ( https://www.rcsb.org/ ). The docking was performed by using software of AutoDock Vina.

Article Snippet: Doxorubicin (HY‐15142A), paclitaxel (HY‐B0015), vincristine (HY‐N0488), topotecan (HY‐13768), and verapamil (HY‐14275) were from supplier of MedChem Express (Monmouth Junction, NJ, USA).

Techniques: Transduction, Binding Assay, Western Blot, Control, Expressing, Incubation, Software

Reporter fluorescence changes in response to topoisomerase inhibitors. Flow cytometry histograms comparing green fluorescence intensities in 17-week-old reporter organoids exposed to A) 1 µM topotecan, B) 1 µM irinotecan, and C) 0.2% DMSO in water (vehicle control). The parental and reporter iPSCs were used to determine the GF +/-gate. a.u. - arbitrary units.

Journal: bioRxiv

Article Title: A Human Angelman Syndrome Class II Pluripotent Stem Cell line with Fluorescent Paternal UBE3A Reporter

doi: 10.1101/2025.07.12.664539

Figure Lengend Snippet: Reporter fluorescence changes in response to topoisomerase inhibitors. Flow cytometry histograms comparing green fluorescence intensities in 17-week-old reporter organoids exposed to A) 1 µM topotecan, B) 1 µM irinotecan, and C) 0.2% DMSO in water (vehicle control). The parental and reporter iPSCs were used to determine the GF +/-gate. a.u. - arbitrary units.

Article Snippet: Topotecan hydrochloride and irinotecan hydrochloride (both from Molcan Corporation) were directly added to 17-week-old AS reporter organoids at a final concentration of 1μM in culture.

Techniques: Fluorescence, Flow Cytometry, Control