| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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TED-347 (TED347) is a novel, covalent/irreversible, and allosteric YAP-TEAD protein-protein interaction inhibitor with anticancer activity. It inhibits TEAD4-Yap1 protein-protein interaction with an EC50 of 5.9 μM. It acts by covalently binding to Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM, thus blocking TEAD transcriptional activity.
| ln Vitro |
The motility of GBM43 sperm is inhibited by TED-347 (0.5-100 μM; 48 hours) [1]. The co-immunoprecipitation of Myc-tagged TEAD4 and FLAG-tagged Yap1 is inhibited by TED-347 (5 μM; 48 hours) [1]. The calibrator levels are significantly reduced in -347 (10 μM; 48 hours) CTGF [1]. Cells transfected with the TEAD reporter gene exhibit decreased reporter activity in response to TED-347 (0.5-100 μM; 24 hours). In GBM43 cells, TED-347 (0.5-100 μM) also suppresses TEAD4 transcriptional activity [1]. TED-347 exhibits the same level of efficacy as TEAD2 inhibition and is selective for TEADs. It has been observed that TED-347 (0.1-100 μM; 24-48 hours) mimicking TED-347 (1-100 μM) did not inhibit Cav2.2 αβ protein-protein reactions or uPAR uPA. The precision of TEAD4 Yap1 binding affinity is impacted by the non-covalent binding of TED-347 to TEAD4 [1]. TED-347 exhibits a response t1/2∞ of 18.2 hours and a maximal inactivation of 0.038 hours [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: GBM43 glioblastoma cell line Tested Concentrations: 0.5, 1, 10, 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited GBM43 cancer cell viability, inhibited GBM43 cell viability by 30% at 10 μM. Western Blot Analysis[1] Cell Types: HEK-293 Cell Tested Concentrations: 5 μM Incubation Duration: 48 hrs (hours) Experimental Results: Significant loss of Myc-tagged TEAD4 co-immunoprecipitated with FLAG-tagged Yap1. RT-PCR[1] Cell Types: HEK-293 Cell Tested Concentrations: 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: CTGF transcript levels were Dramatically diminished compared to control cells and had negative effects on TEAD mutant transcriptional activity and protein-protein interactions Cell culture was not inhibited. |
| References |
[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.
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| Molecular Formula |
C₁₅H₁₁CLF₃NO
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|---|---|
| Molecular Weight |
313.70
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| CAS # |
2378626-29-8
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| Related CAS # |
2378626-29-8;
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| SMILES |
ClC([H])([H])C(C1=C([H])C([H])=C([H])C([H])=C1N([H])C1=C([H])C([H])=C([H])C(C(F)(F)F)=C1[H])=O
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| Synonyms |
TED347 TED 347
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~318.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (19.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 2: 2.5 mg/mL (7.97 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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