| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
STAT3 0.33 μM (IC50)
Ac-GpYLPQTV-NH2 acetate specifically targets the SH2 domain of STAT3, a key transcription factor involved in cell proliferation, survival, and immune responses. By binding to the SH2 domain with high affinity (IC50 = 0.33 microM), it competitively blocks the recruitment of STAT3 to activated receptor complexes. This inhibition prevents STAT3 phosphorylation, dimerization, and nuclear translocation, thereby suppressing the transcription of downstream oncogenes such as Bcl-2, survivin, and cyclin D1. |
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| ln Vitro |
In vitro, Ac-GpYLPQTV-NH2 acetate exhibits potent antiproliferative activity against various cancer cell lines, including breast cancer (MCF-7) and colon cancer (HCT-116) cells. It induces apoptosis in a dose-dependent manner by downregulating anti-apoptotic Bcl-2 gene expression. The IC50 for STAT3 inhibition is 0.33 microM. Importantly, it shows low toxicity toward normal epithelial cells (e.g., HEK293), indicating a favorable therapeutic window.
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| ln Vivo |
Ac-GpYLPQTV-NH2 acetate has demonstrated antitumor activity in in vivo xenograft models. As a STAT3 inhibitor, it is used to explore tumor resistance mechanisms and combination therapy regimens. Its potential for treating STAT3-dependent malignancies, including breast and colon cancers, is supported by preclinical data showing tumor growth inhibition and induction of apoptosis. No specific clinical trial data is available as it is a research reagent.
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| Enzyme Assay |
The binding affinity of Ac-GpYLPQTV-NH2 acetate to the STAT3 SH2 domain is typically assessed using surface plasmon resonance (SPR). Recombinant human STAT3 SH2 domain is immobilized on a CM5 sensor chip. The peptide is injected at varying concentrations (0.01-100 uM) in running buffer (PBS, pH 7.4, 0.05% Tween-20). Association (kon) and dissociation (koff) rates are recorded, and the equilibrium dissociation constant (Kd) is calculated. The IC50 is determined by a competition binding assay using a fluorescently labeled STAT3 phosphopeptide.
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| Cell Assay |
The in vitro antiproliferative activity of Ac-GpYLPQTV-NH2 acetate is measured by the MTT assay. Cancer cells (e.g., MCF-7, HCT-116) are seeded in 96-well plates (5,000-10,000 cells/well) and incubated overnight. The peptide is serially diluted (0.01-100 uM) and added to the cells for 48-72 h. Cell viability is then measured by MTT assay. Apoptosis induction is confirmed by Annexin V-FITC/PI staining and flow cytometry. STAT3 phosphorylation (p-STAT3 Tyr705) and Bcl-2 expression levels are assessed by Western blotting.
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| Animal Protocol |
For in vivo efficacy studies, female BALB/c nude mice (6-8 weeks old, n=6-8/group) are subcutaneously inoculated with 5×10⁶ cancer cells (e.g., MCF-7 or HCT-116). When tumors reach ~100-150 mm3, Ac-GpYLPQTV-NH2 acetate is formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline and administered intraperitoneally at doses of 10-50 mg/kg once daily for 2-3 weeks. Tumor volume is measured every 2-3 days with calipers (volume = length × width2/2). At the endpoint, tumors are excised, weighed, and analyzed for p-STAT3 and Bcl-2 expression by Western blotting or immunohistochemistry (Ki-67 for proliferation, cleaved caspase-3 for apoptosis).
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| ADME/Pharmacokinetics |
Ac-GpYLPQTV-NH2 acetate (MW 897.91, predicted LogP ~0-1) is a moderately polar peptide. Following intraperitoneal or intravenous administration, it may have a short plasma half-life (< 1-2 h) due to proteolytic degradation and renal clearance. The C-terminal amide modification increases stability against carboxypeptidases. For in vitro use, it is soluble in DMSO (10-50 mM). For in vivo studies, it is formulated in 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline. Detailed PK data is limited as it is a research reagent.
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| Toxicity/Toxicokinetics |
Ac-GpYLPQTV-NH2 acetate is a research-grade peptide and should be handled with standard laboratory safety precautions. The peptide may cause skin and eye irritation (H315, H319). It is not intended for human consumption. Potential toxicities are not well-characterized, but as a STAT3 inhibitor, on-target effects may include immune modulation (STAT3 plays a role in immune regulation) and gastrointestinal disturbances. For research use only, use PPE (gloves, lab coat, safety goggles), work in a fume hood, avoid inhalation and skin contact.
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| References | |
| Additional Infomation |
Ac-GpYLPQTV-NH2 acetate is a research-grade STAT3 inhibitor (IC50 = 0.33 uM) used for studying STAT3 signaling pathways in oncology. It is not an FDA-approved drug. It serves as a molecular tool for investigating tumor cell proliferation, apoptosis, and drug resistance mechanisms. It is also used in the development of STAT3-targeted therapeutics and as a reference standard in biochemical assays. For research use only, not for diagnostic or therapeutic applications. Storage: powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 6 months, -20degC for 1 month.
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| Molecular Formula |
C38H60N9O14P.XC2H4O2
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| Molecular Weight |
897.91 (free base)
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| Related CAS # |
Ac-GpYLPQTV-NH2;1349616-70-1
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| Appearance |
White to off-white 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) |
DMSO : ~100 mg/mL (with ultrasonication)
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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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