TED-347 is a potent, irreversible, covalent and allosteric inhibitor of the TEAD-Yap protein-protein interaction. TED-347 inhibits TEAD4-Yap1 interaction with an EC50 value of 5.9 μM.
HazMat Fee +
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Yap1, which binds tightly to TEAD4 via a large flat interface, promotes tumor progression and metastasis through its TEAD-interaction domain. TED-347 is a potent and irreversible covalent allosteric inhibitor of the TEAD⋅Yap interaction. Following 24 hr incubation of TEAD4 with TED-347 at 4 ℃, the compound inhibited the TEAD⋅Yap protein-protein interaction by 53% with an apparent EC50 of 5.9 μM. TED-347 was found to inhibit the protein-protein interaction in a time-dependent manner (0.5, 6, 24, and 48 hr), and it reached maximum inhibition of 80% at 48 hr. In HEK-293 cells transfected with a TEAD reporter, TED-347 (5 μM; 48 hr) resulted in over 70% reduction in reporter activity, whereas cells treated with 10 μM of TED-347 showed a complete loss of reporter activity, suggesting TED-347 inhibits TEAD transcriptional activity and protein-protein interactions in cell culture. Moreover, TED-347 (10 μM) inhibited GBM43 cancer cell viability by 30%[2].
作用机制
TED-347 forms a covalent bond with a conserved Cys-367 located within the unique deep hydrophobic palmitate-binding pocket of TEADs[2].
搜索
HazMat Fee +
