TED-347 是一种有效，不可逆且共价的 YAP-TEAD 蛋白质-蛋白质相互作用变构抑制剂，对 TEAD4•Yap1 蛋白质-蛋白质相互作用的 EC₅₀ 为 5.9 μM。TED-347 与 TEAD4 中央口袋内的 Cys-367 特异性共价结合，K_i 为 10.3 μM。TED-347 可以阻断 TEAD 的转录活性，并且具有抗肿瘤活性。

TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC 50 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.

Solid

IC50: 5.9 μM (TEAD4?Yap1 protein-protein interaction)

TED-347 (0.5-100 μM; 48 hours) inhibits GBM43 cancer cell viability.
TED-347 (5 μM; 48 hours) inhibits co-immunoprecipitation of Myc-tagged TEAD4 with FLAG-tagged Yap1.
TED-347 (10 μM; 48 hours) shows a significant reduction in CTGF transcript levels.
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.
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.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Khuchtumur Bum-Erdene, et al. Small-Molecule Covalent Modification of Conserved Cysteine Leads to Allosteric Inhibition of the TEAD?Yap Protein-Protein Interaction. Cell Chem Biol. 2019 Mar 21;26(3):378-389.e13.

In Vitro: DMSO : 100 mg/mL (318.78 mM; Need ultrasonic)配制储备液