TAU-IN-3 is an orally active inhibitor of tau protein. This compound effectively inhibits the expression of the MAPT exon 10 DDPAC mutant gene in HeLa cells, demonstrating an IC50 of 0.6 µM. It reduces the 4-repeat/3-repeat MAPT mRNA ratio in cells with wild-type or DDPAC minigenes and inhibits the insertion of endogenous MAPT exon 10, subsequently decreasing the production of 4-repeat tau protein. TAU-IN-3 also modulates tau splicing in htau mice, yielding improvements in associated behavioral phenotypes, making it a valuable reagent for studies on neurodegenerative diseases.
TAU-IN-3 is an orally active inhibitor of tau protein. This compound effectively inhibits the expression of the MAPT exon 10 DDPAC mutant gene in HeLa cells, demonstrating an IC50 of 0.6 µM. It reduces the 4-repeat/3-repeat MAPT mRNA ratio in cells with wild-type or DDPAC minigenes and inhibits the insertion of endogenous MAPT exon 10, subsequently decreasing the production of 4-repeat tau protein. TAU-IN-3 also modulates tau splicing in htau mice, yielding improvements in associated behavioral phenotypes, making it a valuable reagent for studies on neurodegenerative diseases.
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