| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
TT-10 targets the YAP-TEAD transcriptional complex, acting as an activator of YAP/TEAD activity. YAP (Yes-associated protein) and TEAD (Transcriptional Enhancer Associate Domain) transcription factors are key downstream effectors of the Hippo signaling pathway. Activation of YAP-TEAD promotes the transcription of genes involved in cell proliferation, survival, and tissue regeneration. By activating this pathway, TT-10 can stimulate cell proliferation and promote tissue repair.
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| ln Vitro |
TT-10 (48 h) significantly enhances the activation of the cell cycle and the proliferation of cardiomyocytes produced from human induced pluripotent stem cells (hiPSCs)[1].
TT-10 activates YAP-TEAD transcriptional activity. The compound's ability to promote YAP/TEAD-mediated transcription has been characterized in cellular assays. By activating YAP signaling, TT-10 can induce cell proliferation in various cell types. Its activity is particularly relevant for studies of tissue regeneration and heart disease, where YAP signaling plays a critical role in cardiomyocyte proliferation and cardiac repair. |
| ln Vivo |
TT-10 can be used for research of heart diseases accompanied by cardiomyocyte loss. By activating YAP-TEAD signaling, the compound promotes cardiomyocyte proliferation and may facilitate cardiac repair. In vivo studies have explored its potential to stimulate regeneration in damaged heart tissue. The compound's ability to activate YAP signaling makes it a valuable tool for studying tissue regeneration and the therapeutic potential of YAP activation in various disease models.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for TT-10 typically involves a transcriptional activity assay using recombinant YAP and TEAD proteins. The YAP-TEAD complex is incubated with a DNA probe containing a TEAD consensus binding sequence and varying concentrations of TT-10. The increase in YAP-TEAD binding to DNA or transcriptional activity is measured using an ELISA-based or electrophoretic mobility shift assay (EMSA). Alternatively, a cell-free transcription assay can be used to measure TEAD-dependent transcription.
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| Cell Assay |
The in vitro cellular assay for TT-10 typically uses cells with measurable YAP-TEAD activity. Cells are treated with varying concentrations of TT-10, and TEAD-dependent transcriptional activity is measured using a TEAD-responsive luciferase reporter assay. Cell proliferation is assessed using standard assays such as BrdU incorporation, EdU labeling, or cell counting. The compound's effects on YAP target gene expression can be evaluated by qPCR or Western blot. In cardiomyocyte models, the compound's effects on proliferation and survival are assessed.
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| Animal Protocol |
In vivo animal studies for TT-10 typically involve models of heart disease accompanied by cardiomyocyte loss. For example, in models of myocardial infarction or heart failure, TT-10 is administered via appropriate routes, and cardiac function, cardiomyocyte proliferation, and tissue regeneration are assessed. The compound's ability to promote YAP-dependent proliferation and repair in damaged heart tissue is evaluated. Specific protocols depend on the animal model and the biological question being addressed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for TT-10 are not extensively reported. The compound has a molecular weight of 283.35 and a formula of C11H10FN3OS2. It is soluble in DMSO. 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 TT-10 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 |
TT-10 (TAZ-K) is an activator of YAP-TEAD activity. It promotes YAP/TEAD-mediated transcription and cell proliferation. The compound is used for research of heart diseases accompanied by cardiomyocyte loss. TT-10 serves as a valuable tool for studying the Hippo signaling pathway, tissue regeneration, and the therapeutic potential of YAP activation. It is not in clinical trials and has not been approved for therapeutic use. It remains an experimental tool for basic research into YAP-TEAD biology and regeneration.
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| Molecular Formula |
C11H10FN3OS2
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|---|---|
| Molecular Weight |
283.345002651215
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| Exact Mass |
283.024
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| CAS # |
2230640-94-3
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| PubChem CID |
134827875
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| Appearance |
Yellow to orange solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
18
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| Complexity |
331
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(=NC(=C1C(C1=CC=C(F)S1)=O)N)NCC=C
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| InChi Key |
GVYPHJQPOHDZEI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H10FN3OS2/c1-2-5-14-11-15-10(13)9(18-11)8(16)6-3-4-7(12)17-6/h2-4H,1,5,13H2,(H,14,15)
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| Chemical Name |
[4-amino-2-(prop-2-enylamino)-1,3-thiazol-5-yl]-(5-fluorothiophen-2-yl)methanone
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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 |
| 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: 50 mg/mL (176.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.82 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 (8.82 mM) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5292 mL | 17.6460 mL | 35.2920 mL | |
| 5 mM | 0.7058 mL | 3.5292 mL | 7.0584 mL | |
| 10 mM | 0.3529 mL | 1.7646 mL | 3.5292 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.
Link: https://clinicaltrials.gov/ct2/show/NCT04969315
Conditions:Renal Cell Cancer|Castrate Resistant Prostate Cancer|Non Small Cell Lung Cancer|Head and Neck Squamous Cell Carcinoma|Colorectal Cancer (CRC)|Endometrial Cancer|Ovarian CancerProducts are for research use only; We do not sell to patients
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