The transcriptional coactivator Yes-associated protein (YAP) is a major regulator of organ size and proliferation in vertebrates. As such, YAP can act as an oncogene in several tissue types if its activity is increased aberrantly. YAP enhances multiple processes known to be important for tumor progression and metastasis, including cellular proliferation, transformation, migration, and invasion.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H6007 |
TED-347 |
2378626-29-8 |
TED-347 (TED347) is an irreversible inhibitor of TEAD4-Yap1 protein-protein interaction (EC50=5.9 uM in FP asssays) via covalent modification of conserved cysteine (Cys367, Ki=1.3 uM), inhibits its binding to Yap1, blocked its transcriptional activity; inhibits TEAD transcriptional activity and protein interactions in cells at 5 uM resulted in over 70% reduction in reporter activity; inhibits GBM43 cancer cell viability by 30% at 10 uM, also inhibits TEAD4 transcriptional activity in GBM43 cells. |
H6006 |
IBS003031 |
381177-81-7 | IBS003031 (IBS-003031) is a novel chemical Yes-associated protein 1 (YAP1) activator, up-regulates H2B-mCherry expression at 1 and 3 uM in mCherry signal based reporter assays; remarkably increased the amount of unphosphorylated YAP1 and decreased that of phosphorylated YAP1, enhanced the expression of YAP1 target genes, CTGF and CYR61, in U2OS cells; does not inhibits LATS1/2 activities or blocks the interaction of YAP1 and LATS kinases; decreased the viability in the dose-dependent manner in MM cells and enhanced Bax expression, increased p73-dependent transcription MDM2, FAS, and BAX in mRNA level. |
H6009 |
Verteporfin |
129497-78-5 | Verteporfin (CL 318952, BPD-MA) is a benzoporphyrin derivative that inhibits Yap via disruption of YAP-TEAD interactions, Verteporfin is a clinically used photosensitizer; inhibits growth of hepatoma cells without photoactivation through inhibition of YAP-TEAD complex; inhibited tumor cell proliferation and restored sensitivity to cisplatin in urothelial cell carcinoma (UCC); blocks tumor growth of uveal melanoma cells containing Gq/11 mutations. |
H6008 |
TT-10 |
2230640-94-3 | TT-10 (YAP-TEAD activator TT-10) is a small molecule activator that activates pro-proliferative YES-associated protein (YAP) and transcriptional enhancer factor domain (TEAD) activities in cardiomyocytes; promoted cardiomyocyte proliferation and simultaneously exerted antioxidant and antiapoptotic effects in vitro via nuclear translocation of YAP, activates YAP-TEADs activity and the Wnt/β-Catenin signaling pathway; ameliorates cardiac dysfunction, decreases ROS and DNA aamage and apoptosis after myocardial infarction (MI) in mice. |
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