1. Stem Cell/Wnt
  2. YAP
  3. TED-347

TED-347 

Cat. No.: HY-125269
Handling Instructions

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.

For research use only. We do not sell to patients.

TED-347 Chemical Structure

TED-347 Chemical Structure

CAS No. : 2378626-29-8

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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].

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 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.
Molecular Weight

313.70

Formula

C₁₅H₁₁ClF₃NO

CAS No.

2378626-29-8

SMILES

O=C(C1=CC=CC=C1NC2=CC=CC(C(F)(F)F)=C2)CCl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (796.94 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1878 mL 15.9388 mL 31.8776 mL
5 mM 0.6376 mL 3.1878 mL 6.3755 mL
10 mM 0.3188 mL 1.5939 mL 3.1878 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (19.92 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TED-347TED347TED 347YAPYes-associated proteinirreversiblecovalentallostericYAP-TEADprotein-proteininteractionTEAD4?Yap1Cys-367TEAD4TEADtranscriptionalantitumorYap1glioblastomaPPIInhibitorinhibitorinhibit

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Product name:
TED-347
Cat. No.:
HY-125269
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