Antitumor agent-171 is a potent inhibitor of the β-catenin/BCL9 interaction, demonstrating an IC50 value of 1.61 μM. This compound exhibits a strong binding affinity to β-catenin, with a Kd of 0.63 μM, and effectively inhibits the expression of the axin2 gene with an IC50 of 0.84 μM. Additionally, Antitumor agent-171 reduces cell viability in HCT116 cells at an IC50 of 4.39 μM. Its ability to activate T cells and enhance antigen presentation underscores its potential in antitumor applications, with favorable pharmacokinetic properties observed in mouse models.
Antitumor agent-171 is a potent inhibitor of the β-catenin/BCL9 interaction, demonstrating an IC50 value of 1.61 μM. This compound exhibits a strong binding affinity to β-catenin, with a Kd of 0.63 μM, and effectively inhibits the expression of the axin2 gene with an IC50 of 0.84 μM. Additionally, Antitumor agent-171 reduces cell viability in HCT116 cells at an IC50 of 4.39 μM. Its ability to activate T cells and enhance antigen presentation underscores its potential in antitumor applications, with favorable pharmacokinetic properties observed in mouse models.
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