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Biological Activity:

Verteporfin (Visudyne) is a potent and selective YAP inhibitor, disrupts YAP-TEAD interactions and enhances trypsin cleavage of YAP with EC50 ~100 nM. It inhibits growth and proliferation of retinoblastoma cells. It also significantly blocks cancer stem cell (CSC) properties in cells with high YAP1 and a high proportion of ALDH1(+). In vivo it can suppress YAP-induced liver overgrowth in mice.

How to Use:

In vitro: Verteporfin was used at 10 μM final concentration in various in vitro assays.
In vivo: Verteporfin was administered by intraperitoneal injection at 100 mg/Kg once every other day in liver overgrowth model.

Reference:

• 1. Liu-Chittenden Y, et al. Genetic and pharmacological disruption of the TEAD-YAP complex suppresses the oncogenic activity of YAP. (2012) Genes Dev. 26(12):1300-5.?
• 2. Brodowska K, et al. The clinically used photosensitizer Verteporfin (VP) inhibits YAP-TEAD and human retinoblastoma cell growth in vitro without light activation. (2014) Exp Eye Res. 124:67-73.?
• 3. Song S, et al. Hippo coactivator YAP1 upregulates SOX9 and endows esophageal cancer cells with stem-like properties. (2014) Cancer Res. 74(15):4170-82.?