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. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a K_i of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity^[1]. IC50 & Target: IC50: 5.9 μM (TEAD4?Yap1 protein-protein interaction)^[1] In Vitro: TED-347 (0.5-100 μM; 48 hours) inhibits GBM43 cancer cell viability^[1].
TED-347 (5 μM; 48 hours) inhibits co-immunoprecipitation of Myc-tagged TEAD4 with FLAG-tagged Yap1^[1].
TED-347 (10 μM; 48 hours) shows a significant reduction in CTGF transcript levels^[1].
TED-347 (0.5-100 μM; 24 hours) reduces reporter activity in cells transfected with a TEAD reporter. TED-347 (0.5-100 μM) also inhibits TEAD4 transcriptional activity in GBM43 cells^[1].
TED-347 is selective for TEADs and inhibits TEAD2 with the same efficacy. TED-347 (0.1-100 μM; 24-48 hours) inhibits TEAD4 binding to full-length Yap1 in dose- and time-dependent manner. TED-347 (1-100 μM) shows no inhibition of uPAR?uPA or Cav2.2 α?β protein-protein interactions. Non-covalent binding of TED-347 to TEAD4 exhibits little change to the TEAD4?Yap1 binding affinity^[1].
TED-347 has the maximum rate of inactivation of 0.038 hours, corresponding to a t_1/2^∞ of 18.2 hours^[1].