2378626-29-8
2378626-29-8 structure
- Name: TED-347
- Chemical Name: TED-347
- CAS Number: 2378626-29-8
- Molecular Formula: C15H11ClF3NO
- Molecular Weight: 313.70
- Catalog: Signaling Pathways Stem Cell/Wnt YAP
- Create Date: 2020-06-01 08:32:23
- Modify Date: 2024-01-13 18:23:02
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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 Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity[1].
| Name | TED-347 |
|---|
| Description | 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 Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity[1]. |
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| Related Catalog | |
| 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 t1/2∞ of 18.2 hours[1]. Cell Viability Assay[1] Cell Line: GBM43 glioblastoma cell lines Concentration: 0.5, 1, 10, 100 μM Incubation Time: 48 hours Result: Inhibited GBM43 cancer cell viability and inhibited GBM43 cell viability by 30% at 10 μM. Western Blot Analysis[1] Cell Line: HEK-293 cells Concentration: 5 μM Incubation Time: 48 hours Result: Showed a significant loss of co-immunoprecipitation of Myc-tagged TEAD4 with FLAG-tagged Yap1. RT-PCR[1] Cell Line: HEK-293 cells Concentration: 10 μM Incubation Time: 48 hours Result: Showed a significant reduction in CTGF transcript levels versus control cells and had no inhibition on TEAD mutant transcriptional activity and protein-protein interactions in cell culture. |
| References |
| Molecular Formula | C15H11ClF3NO |
|---|---|
| Molecular Weight | 313.70 |