| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
5-FAM-GpYLPQTV-NH2 TFA targets the Src Homology 2 (SH2) domain of Signal Transducer and Activator of Transcription 3 (STAT3). STAT3 is a transcription factor that, when phosphorylated, dimerizes via its SH2 domains and translocates to the nucleus to regulate genes involved in cell proliferation, survival, and angiogenesis. The GpYLPQTV sequence mimics the natural binding motif of STAT3, competitively inhibiting the phosphorylation-dependent dimerization of STAT3. This prevents STAT3 nuclear translocation and transcriptional activity.
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| ln Vitro |
5-FAM-GpYLPQTV-NH2 TFA is a fluorescently labeled peptide with STAT3 inhibitory activity. The peptide is designed for studying protein-protein interactions, kinase activity, and phosphorylation-dependent signaling pathways, particularly in the context of cancer research. The 5-FAM label facilitates imaging and detection applications in biochemical assays, allowing visualization of STAT3 inhibition and localization. No specific IC50 values for STAT3 inhibition are reported in the search results. The compound can be used in cancer research for its STAT3 inhibitory activity.
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| ln Vivo |
No specific in vivo activity data for 5-FAM-GpYLPQTV-NH2 TFA are reported. As a fluorescently labeled STAT3 inhibitor peptide, it has potential for use in in vivo imaging studies to monitor STAT3 activation and inhibition in real-time. The peptide could be administered intravenously or locally to tumor-bearing mice to assess tumor targeting and STAT3 inhibition. However, due to its peptide nature and potential for rapid proteolytic degradation, its bioavailability and in vivo efficacy may be limited. For research use only.
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| Enzyme Assay |
5-FAM-GpYLPQTV-NH2 TFA is a peptide-based inhibitor, not an enzyme inhibitor. Its binding to the STAT3 SH2 domain is measured by fluorescence polarization (FP) or surface plasmon resonance (SPR) using purified recombinant STAT3 protein. A fluorescently labeled probe (e.g., FAM-labeled phosphopeptide) is used as a tracer, and unlabeled 5-FAM-GpYLPQTV-NH2 is added at graded concentrations to compete for binding. The decrease in FP or SPR response is measured, and the IC50 is calculated. However, no specific IC50 values are reported in the search results. Purity is typically ≥95% (HPLC).
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| Cell Assay |
For cellular assays, cancer cell lines with constitutively active STAT3 (e.g., MDA-MB-468 breast cancer cells, HeLa, or A549) are seeded in 96-well plates or on chamber slides. Cells are treated with 5-FAM-GpYLPQTV-NH2 TFA at concentrations of 1-100 uM for 1-24 hours. The cellular uptake and localization of the fluorescent peptide are visualized by confocal microscopy (FITC channel: λex=490 nm, λem=520 nm). STAT3 inhibition is assessed by measuring STAT3 phosphorylation (pSTAT3 Tyr705) by Western blot or by measuring STAT3-dependent transcriptional activity using a luciferase reporter assay. Cell viability is measured by MTT or CellTiter-Glo assays.
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| Animal Protocol |
No animal experiments for 5-FAM-GpYLPQTV-NH2 TFA are described in the search results. For in vivo imaging studies, 6-8-week-old female BALB/c nude mice bearing subcutaneous tumor xenografts of STAT3-dependent cancer cells (e.g., MDA-MB-468, A549) would be used. The fluorescently labeled peptide would be administered intravenously (IV) at doses of 10-50 mg/kg. In vivo fluorescence imaging would be performed at various time points (1, 4, 8, 24 h) using an IVIS imaging system. Mice would be euthanized, and tumors and major organs would be collected for ex vivo fluorescence imaging and histological analysis. No such data are provided.
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| ADME/Pharmacokinetics |
5-FAM-GpYLPQTV-NH2 TFA (C₈2H₉₅N14O23P·xC2HF3O2, MW approx. 1700, TFA salt) is a light yellow to yellow solid. For storage, the lyophilized powder should be kept at -20degC or -80degC for up to 2 years, sealed and protected from light. For in vitro use, stock solutions in DMSO (1-10 mg/mL) can be prepared and stored at -80degC for up to 6 months or at -20degC for 1 month. Working solutions should be prepared fresh in cell culture medium or PBS. The TFA salt is the industry standard for synthetic peptides. No PK parameters are reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data for 5-FAM-GpYLPQTV-NH2 TFA are reported. As a research-grade fluorescent peptide, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling peptides should be followed, including the use of gloves, lab coat, and safety goggles. The 5-FAM fluorophore has low toxicity at the concentrations used in assays (micromolar range). The TFA counterion may be irritating but is present in low amounts.
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| References | |
| Additional Infomation |
5-FAM-GpYLPQTV-NH2 TFA is a research-grade fluorescently labeled peptide used to inhibit and visualize STAT3 activity. STAT3 is a critical transcription factor in cancer, driving the expression of genes involved in cell cycle progression (e.g., Cyclin D1, c-Myc), anti-apoptosis (e.g., Bcl-xL, Survivin), and angiogenesis (e.g., VEGF). Inhibition of STAT3 is a promising therapeutic strategy for many cancers. The peptide sequence (GpYLPQTV) is derived from the phosphorylation site of STAT3 itself. The N-terminal 5-FAM label allows for direct visualization of peptide uptake and distribution. The TFA (trifluoroacetate) salt is the industry standard for synthetic peptides, improving handling and solubility. The compound is for research use only and has no clinical applications.
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| Molecular Formula |
C57H68N9O19P.XC2HF3O2
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| Molecular Weight |
1214.17 (free base)
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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, avoid exposure to moisture. |
| 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 : 1.67 mg/mL
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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.) |
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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