TABLE 1.
YAP/TAZ nuclear shuttling inhibitors
| Molecule | Other name(s) | Inhibitory action | Binding validation | Activity validation | Binding affinity (KD) | IC50 | Reference(s) | Vendor |
|---|---|---|---|---|---|---|---|---|
| Verteporfin | Visudyne | Inhibitor of YAP nuclear localization | NR | Co‐IP, TEAD luciferase reporter, PLA, YAP‐TEAD target gene qPCR | NR | 8 nM–11.16 μM (Cell line‐dependent) | 184, 185, 195 |
Selleckchem (#S1786) Tocris (#5305) |
| A35 | CHEMBL3041188 | YAP S127 phosphorylation agonist | NR | WB | NR |
<1 μM (Cell line‐dependent) |
190 | |
| Dichloroacetate | Dichloroacetic acid salt | Inhibitor of YAP nuclear localization (Hippo‐dependent) | NR | IFM, WB, RNA‐seq, TEAD luciferase reporter, YAP‐TEAD target gene qPCR | NR | 80–183 μM | 191 |
Selleckchem (#S8615) |
| Dasatinib | Sprycel | Inhibitor of YAP nuclear localization (tyrosine kinase dependent) | NR | IFM, TEAD luciferase reporter, WB, YAP‐TEAD target gene qPCR | NR | ~1 nM | 130 |
Selleckchem (#S1021) Merck (#SML2589) |
| Pazopanib | YAP phosphorylation agonist and promotes proteasomal degradation | NR | IFM, TEAD luciferase reporter, WB | NR | <15 μg/ml | 199 |
Merck (#SML3104) |
|
| CA3 | CIL56 | Inhibitor of YAP expression | NR | IFM, TEAD luciferase reporter, WB, YAP‐TEAD target gene qPCR | NR |
<1 μM (Cell line dependent) |
194, 195 |
Selleckchem (#S8661) |
|
Statins: Cerivastatin Mevastatin Simvastatin Fluvastatin |
Brand names: Baycol Compactin Zocor Lescol |
Inhibitors of YAP nuclear localization via mevalonate pathway (HMG‐CoA reductase) | NR | IFM, TEAD luciferase reporter, WB, YAP‐TEAD target gene qPCR | NR |
<10 μM ~26 nM ~6 μM >0.8 μM (Cell line‐dependent) |
198, 199, 200, 239 |
Merck (#SML0005) (#M2537) (#S6196) (#SML0038) |
|
PI3K‐AKT/PDK1 signalling inhibitors: LY294002 – PI3Ki AKT inhibitor V – AKTi PDK1 inhibitor II – PDK1i Wortmannin – PI3Ki AKT inhibitor VIII – AKTi Calphostin C – PKCi Gö 6983 – PKCi BX795 – PDK1i, TBK1i |
Triciribine | YAP phosphorylation agonists via PDK1‐Hippo‐dependent activity | NR | IFM, YAP‐TEAD target gene qPCR | NR |
<10 μM <20 μM 6 nM 2–4 nM 0.058–2.12 μM 50 nM 6–60 nM 6 nM |
136, 138, 204 |
Merck (#L9908) (#124038) (#521276) (#W1628) (#124017) (#C6303) (#G1918) Santa‐Cruz (#sc‐281 689) |
Abbreviations: Co‐IP, co‐immunoprecipitation; IFM, immunofluorescence microscopy; NR, not reported; PLA, proximity ligation assay; WB, Western blotting.