| Size | Price | Stock | Qty |
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| Other Sizes |
| Targets |
DC-TEADin02 targets TEAD transcription factors by inhibiting their autopalmitoylation, a post-translational modification that is required for TEAD function. Autopalmitoylation of TEAD is essential for its stability and transcriptional activity. DC-TEADin02 is a vinylsulfonamide derivative that covalently modifies TEAD, preventing autopalmitoylation and thereby blocking TEAD activity. This inhibits the interaction between TEAD and YAP/TAZ coactivators and suppresses TEAD-dependent transcription.
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| ln Vitro |
DC-TEADin02 inhibits TEAD autopalmitoylation with an IC50 value of 197 nM[1]. The downregulation of downstream gene expression related to YAP is caused by the inhibition of TEAD transcriptional activity by DC-TEADin02 (0-25 μM) [1].
DC-TEADin02 inhibits TEAD autopalmitoylation with an IC50 of 197 nM. As a potent inhibitor of TEAD autopalmitoylation, it effectively blocks TEAD activity and downstream YAP/TAZ-TEAD signaling. The compound's covalent mechanism of action provides sustained inhibition of TEAD. In vitro studies have characterized its effects on TEAD autopalmitoylation, TEAD-dependent transcription, and cell proliferation in various cell models. |
| ln Vivo |
In vivo activity data for DC-TEADin02 are not extensively reported. The compound can be used for research of development, regeneration, and tissue homeostasis. By inhibiting TEAD activity, DC-TEADin02 may affect processes such as organ development, tissue regeneration, and stem cell maintenance. Further research is needed to evaluate its efficacy in animal models and to explore its potential applications in developmental biology and regenerative medicine.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for DC-TEADin02 typically involves a TEAD autopalmitoylation assay. Recombinant TEAD protein is incubated with palmitoyl-CoA and varying concentrations of DC-TEADin02. The incorporation of palmitate into TEAD is measured using radiolabeled palmitoyl-CoA or a fluorescence-based detection method. The compound's ability to covalently modify TEAD can be confirmed by mass spectrometry. Inhibition of TEAD autopalmitoylation results in a decrease in palmitate incorporation.
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| Cell Assay |
The in vitro cellular assay for DC-TEADin02 typically uses cells with active YAP/TAZ-TEAD signaling. Cells are treated with varying concentrations of DC-TEADin02, and TEAD-dependent transcriptional activity is measured using a TEAD-responsive luciferase reporter assay. TEAD autopalmitoylation in cells can be assessed using metabolic labeling with a palmitate analog followed by click chemistry and detection. Cell proliferation and viability are assessed using standard assays such as CellTiter-Glo or MTT.
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| Animal Protocol |
In vivo animal studies for DC-TEADin02 are not extensively documented. For TEAD inhibitors in general, common in vivo models include xenograft tumor models in mice or models of development and regeneration. However, specific protocols for DC-TEADin02 in animal models have not been reported in the available literature. Researchers should design appropriate experiments based on the compound's properties and the biological question being addressed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for DC-TEADin02 are not available in the public domain. The compound has a molecular weight of 323.41 and a formula of C19H17NO2S. As a research tool, detailed ADME parameters including absorption, distribution, metabolism, and excretion have not been characterized. Researchers should perform their own pharmacokinetic studies if in vivo application is intended.
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| Toxicity/Toxicokinetics |
Toxicity data for DC-TEADin02 are not available in the public domain. As a research compound, comprehensive toxicological evaluations have not been performed. The compound is intended for laboratory research use only and should be handled with standard safety precautions. Appropriate personal protective equipment should be worn when handling this compound. Consult the Material Safety Data Sheet for specific safety and handling information.
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| References | |
| Additional Infomation |
DC-TEADin02 is a potent, covalent inhibitor of TEAD autopalmitoylation with an IC50 of 197 nM. It is a vinylsulfonamide derivative that covalently modifies TEAD, blocking its autopalmitoylation and activity. The compound can be used for research of development, regeneration, and tissue homeostasis. DC-TEADin02 is not in clinical trials and has not been approved for therapeutic use. It remains a research tool for studying TEAD biology and the Hippo signaling pathway.
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| Molecular Formula |
C19H17NO2S
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|---|---|
| Molecular Weight |
323.41
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| Exact Mass |
323.097
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| CAS # |
2380228-45-3
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| PubChem CID |
155527561
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| Appearance |
White to off-white solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
488
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(S(NC1=CC=C(CC2=CC=C3C(=C2)C=CC=C3)C=C1)(=O)=O)=C
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| InChi Key |
IUZGUIPYVGPQFT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17NO2S/c1-2-23(21,22)20-19-11-8-15(9-12-19)13-16-7-10-17-5-3-4-6-18(17)14-16/h2-12,14,20H,1,13H2
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| Chemical Name |
N-[4-(naphthalen-2-ylmethyl)phenyl]ethenesulfonamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (309.21 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0921 mL | 15.4603 mL | 30.9205 mL | |
| 5 mM | 0.6184 mL | 3.0921 mL | 6.1841 mL | |
| 10 mM | 0.3092 mL | 1.5460 mL | 3.0921 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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