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Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin (CL 318952) is a YAP inhibitor that disrupts YAP-TEAD interactions, and it is also an inhibitor of autophagy that blocks autophagy at an early stage by inhibiting autophagosome formation.
Verteporfin is specifically selected by PDX-cell screening. The concentrations to cause 50% growth inhibition (GI50) for PhLO, PhLH, and PhLK are 228 nM, 395 nM, and 538 nM, respectively, whereas GI50 for ALL-1, TCC-Y/sr, and NPhA1 are 3.93 µM, 2.11 µM, and 5.61 µM, respectively. GSH significantly reduces the sensitivity of 2 out of 3 PDX cells to verteporfin. Verteporfin reduces the mitochondrial membrane potential in PDX cells.
Verteporfin reduces the PTX-resistance on HCT-8/T cells by inhibiting YAP expression and combination therapy with verteporfin and NSC 125973 shows synergism on inhibition of YAP and cytotoxicity to HCT-8/T.
| Cell Experiment | |
|---|---|
| Cell lines | GBM cells |
| Preparation method | To investigate VP activation a Lumenis Opal PDT Laser with Haag slit lamp adapter containing a laser system diode with continuous-wave solid-state laser, the wavelength of 689 ± 3 nm, was used, which is usually applied for PDT with VP at the Department of Ophthalmology, University Hospital Düsseldorf, Germany. GBM cells were applied into black-walled, glass-bottom 96-well plates and subsequently treated with VP in varying concentrations (0.001; 0.01; 0.1; 1 μM) or medium without VP for 24 h. |
| Concentrations | 0.001; 0.01; 0.1; 1 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Female mice |
| Formulation | DMSO |
| Dosages | 6 mg/kg, 10 mg/kg, and 100 mg/kg |
| Administration | Intraperitoneal injection (i.p.) |
| Molecular Weight | 718.79 |
| Formula | C41H42N4O8 |
| CAS Number | 129497-78-5 |
| Solubility (25°C) | DMSO 50 mg/mL DMF 10 mg/mL (ultrasonic and warming) |
| Storage | 2-8°C, protect from light |
| Related YAP Products |
|---|
| YAP-TEAD-IN-1 TFA
YAP-TEAD-IN-1 TFA is a competitive inhibitor of YAP-TEAD interaction with IC50 of 25 nM. |
| Super-TDU
Super-TDU is a specific YAP antagonist that targets YAP-TEAD interactions. Super-TDU can inhibit tumor growth in mouse models of gastric cancer. |
| TED-347
TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. |
| YAP/TAZ inhibitor-1
YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor with an IC50 of <0.100 μΜ in firefly luciferase assay. |
| MYF-01-37
MYF-01-37 is a novel covalent inhibitor of TEAD targeting Cys380 when incubated with the TEAD2 protein. |
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