2136579-33-2

2136579-33-2 structure
2136579-33-2 structure
  • Name: AKR1B10-IN-1
  • Chemical Name: AKR1B10-IN-1
  • CAS Number: 2136579-33-2
  • Molecular Formula: C19H16FNO4
  • Molecular Weight: 341.33
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Aldose Reductase
  • Create Date: 2022-02-20 15:06:19
  • Modify Date: 2025-08-25 16:02:24
  • AKR1B10-IN-1 is a potent inhibitor of AKR1B10 (Aldo-Keto Reductase 1B10) with an IC50 of 3.5 nM. AKR1B10-IN-1 suppresses proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells[1].

Name AKR1B10-IN-1
Synonyms N-(3-(4-Fluorophenyl)propyl) -7-hydroxycoumarin-3-carboxamide
Description AKR1B10-IN-1 is a potent inhibitor of AKR1B10 (Aldo-Keto Reductase 1B10) with an IC50 of 3.5 nM. AKR1B10-IN-1 suppresses proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells[1].
Related Catalog
Target

3.5 nM (AKR1B10); 277 nM (AKR1B1)[1]

In Vitro AKR1B10-IN-1 (compound 4e) (0-20 μM; 96 hours) dose-dependently suppresses the growth of both A549 and A549/1B10 cells[1]. AKR1B10-IN-1 (compound 4e) (0-20 μM; 96 hours) completely suppresses increased cell proliferation by the overexpressing AKR1B10 as well as the endogenous protein[1]. AKR1B10-IN-1 (compound 4e) (0-40 μM; 26 hours; pretreatment with AKR1B10-IN-1 for 2 hours, then incubated with CDDP for 24 hours) decreases the cell viability of CDDP-R-A549 cells in a dose-dependent manner[1]. Cell Viability Assay[1] Cell Line: A549 cells, A549/1B10 cells (AKR1B10-stably overexpressing A549 cells) Concentration: 0, 10, 20 μM Incubation Time: 96 hours Result: Dose-dependently suppressed the growth of both A549 and A549/1B10 cells, and statistically significant at 20 μM. Cell Viability Assay[1] Cell Line: CDDP-resistance (cisplatin-resisitance) of A549 cells Concentration: 0, 10, 20, 40 μM Incubation Time: Pretreatment with AKR1B10-IN-1 for 2 hours, then incubated with CDDP for 24 hours Result: Decreased the cell viability of CDDP-R-A549 cells in a dose-dependent manner, and most obvious in the treatment of 40 μM.
References

[1]. Endo S, et al. Synthesis of Potent and Selective Inhibitors of Aldo-Keto Reductase 1B10 and Their Efficacy against Proliferation, Metastasis, and Cisplatin Resistance of Lung Cancer Cells [published correction appears in J Med Chem. 2018 Feb 8;61(3):1380]. J Med Chem. 2017;60(20):8441-8455.

Molecular Formula C19H16FNO4
Molecular Weight 341.33
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