In vitro activity: IQ-1 is a cell-permeable tetrahydroisoquinolinylidene small molecule compound that modulates Wnt/beta-catenin signaling. IQ-1 was identified from a high-throughput cell-based assay and has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on. IQ-1 binds to serine/threonine phosphatase PP2A and prevents PP2A/Nkd interaction. IQ-1 allows for the Wnt/beta-catenin-driven long-term expansion of mouse ESCs and prevents spontaneous differentiation. IQ-1, by targeting the PR72/130 subunit of the serine/threonine phosphatase PP2A, prevents beta-catenin from switching coactivator usage from CBP to p300. The increase in beta-catenin/CBP-mediated transcription at the expense of beta-catenin/p300-mediated transcription is critical for the maintenance of murine stem cell pluripotency.

Kinase Assay: IQ 1 decreased Wnt-stimulated phosphorylation of p300 at Ser-89.IQ-1 binds to serine/threonine phosphatase PP2A and prevents PP2A/Nkd interaction.The binding of IQ 1 to PR72/130 leads to decreased phosphorylation of the coactivator protein p300 at Ser-89. IQ 1 thereby diminishes the β-catenin/p300 interaction and prevents β-catenin coactivator switching from CBP to p300. I

Cell Assay: IQ-1 was identified from a high-throughput cell-based assay and has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on. IQ-1 binds to serine/threonine phosphatase PP2A and prevents PP2A/Nkd interaction.