| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
YAP-TEAD complex. Super-TDU (1-31) TFA is an inhibitor of the YAP-TEAD interaction. By binding to YAP, it prevents the association of YAP with the TEAD transcription factor, thereby blocking the transcriptional activity of the Hippo pathway. This inhibition suppresses cell proliferation and induces apoptosis in YAP-dependent cancers.
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| ln Vitro |
Super-TDU(1-31) TFA (50 nM; 24-72 hours) can significantly reduce the increase in cell viability in Huh-7 or LM3 cell proliferation that is produced by ACTN1 [1].
Super-TDU (1-31) TFA (50 nM, 24-72 h) largely compromises ACTN1-induced cell viability increases in liver cancer cell lines, including Huh-7 and LM3 cells. By disrupting YAP-TEAD complex formation, it inhibits the transcription of YAP target genes involved in cell proliferation and survival. The peptide demonstrates selective inhibitory activity against YAP-dependent cancer cell proliferation. |
| ln Vivo |
Super-TDU (1-31) TFA shows potent anti-tumor activity in a gastric cancer mouse model, inhibiting tumor growth. Administration of Super-TDU TFA leads to suppression of tumor progression and reduced tumor volume. The in vivo efficacy supports the therapeutic potential of targeting the YAP-TEAD complex with peptide inhibitors for the treatment of cancers driven by hyperactive Hippo signaling.
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| Enzyme Assay |
YAP-TEAD binding inhibition assay (SPR or ELISA): Recombinant YAP protein is immobilized on a sensor chip or ELISA plate. Increasing concentrations of Super-TDU (1-31) TFA (0-1000 nM) are pre-incubated with TEAD protein. The mixture is injected, and the amount of bound TEAD is detected by specific antibodies. Alternatively, a fluorescence polarization assay using labeled TEAD peptide and purified YAP can be used.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Liver cancer cell lines of human, including Huh-7, LM3 cells Tested Concentrations: 50 nM Incubation Duration: 24, 48 and 72 h Experimental Results: Could largely compromise the increased cell viability induced by ACTN1. Cell viability assay: Human liver cancer cells (Huh-7 or LM3) are seeded in 96-well plates (5,000 cells/well) and treated with Super-TDU (1-31) TFA at concentrations of 0-500 nM for 24-72 h. Cell viability is assessed using CCK-8 or MTT assay. For mechanism studies, cells are treated with 50 nM peptide for 48 h, and YAP target gene expression (CTGF, CYR61, ANKRD1) is measured by qRT-PCR. |
| Animal Protocol |
Gastric cancer xenograft model: Female BALB/c nude mice (6-8 weeks old) are subcutaneously implanted with gastric cancer cells (5×10⁶ cells/mouse). When tumors reach ~100 mm3, mice are randomized into groups (n=6-8). Super-TDU (1-31) TFA is administered via intratumoral injection or intraperitoneally at doses of 5-20 mg/kg, every other day for 2-3 weeks. Tumor volume is measured every 3 days using calipers. TUNEL and Ki-67 staining are performed on tumor sections.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Super-TDU (1-31) TFA are limited. As a 31-amino acid peptide (MW 3355.5, TFA salt), it has poor oral bioavailability and a short plasma half-life (typically minutes) due to proteolytic degradation. It is administered via intratumoral or intraperitoneal injection for in vivo studies. The powder should be stored at -20degC, sealed and away from light and moisture.
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| Toxicity/Toxicokinetics |
Toxicity data for Super-TDU (1-31) TFA are limited. As a peptide disrupting the YAP-TEAD interaction, it is intended for research use only and not for human therapeutic applications. In mouse xenograft models at effective doses (5-20 mg/kg, every other day), no significant body weight loss or gross toxicity has been reported. Standard safety precautions should be followed.
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| References | |
| Additional Infomation |
Super-TDU (1-31) TFA is a research compound that has not entered clinical trials or received regulatory approval for human use. It is derived from Super-TDU, which is based on the YAP-binding domain of TEAD. This peptide is a valuable tool for studying Hippo signaling and for validating YAP as a therapeutic target in cancer. For research use only. Sequence shortening: SVDDHFAKSLGDTWLQIGGSGNPKTANVPQT.
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| Molecular Formula |
C141H218N40O48.C2HF3O2
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| Molecular Weight |
3355.50
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| Related CAS # |
Super-TDU (1-31)
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| Appearance |
Solid powder
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O :~50 mg/mL (~14.90 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2980 mL | 1.4901 mL | 2.9802 mL | |
| 5 mM | 0.0596 mL | 0.2980 mL | 0.5960 mL | |
| 10 mM | 0.0298 mL | 0.1490 mL | 0.2980 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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