| 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 |
Caffeic acid-pYEEIE TFA targets the SH2 (Src Homology 2) domain of Src family kinases, specifically binding to the GST-Lck-SH2 domain and the Src SH2 domain. SH2 domains are protein interaction modules that recognize phosphorylated tyrosine residues. This non-phosphopeptide inhibitor was designed by replacing the phosphotyrosine residue with caffeic acid, resulting in a non-phosphorylated scaffold that still binds to the SH2 domain with high affinity (IC₅0 = 42 nM).
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| ln Vitro |
In vitro, Caffeic acid-pYEEIE TFA exhibits potent binding affinity for the GST-Lck-SH2 domain in biochemical binding assays. It is a phosphopeptide ligand for the src SH2 domain with an IC₅0 of 42 nM, showing approximately 30-fold more binding activity than Ac-pYEEIE. The compound is not typically used in cell viability assays, as it is a biochemical tool for studying SH2 domain-protein interactions rather than a modulator of biological pathways in whole cells.
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| ln Vivo |
Detailed in vivo activity data for Caffeic acid-pYEEIE TFA are not reported in standard product literature. As a phosphopeptide inhibitor that targets SH2 domains, it is primarily designed for in vitro biochemical studies to understand protein-protein interactions in cell signaling pathways. Its charged nature and peptidic structure would likely limit membrane permeability, making in vivo applications challenging. No animal model data are available.
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| Enzyme Assay |
Binding affinity of Caffeic acid-pYEEIE TFA for SH2 domains is determined using non-cellular assays such as surface plasmon resonance (SPR) or fluorescence polarization (FP). In an SPR assay, recombinant SH2 domain protein (e.g., GST-Lck-SH2) is immobilized on a sensor chip. Various concentrations of the compound are flowed over the chip, and the association and dissociation rates are monitored to calculate the equilibrium dissociation constant (KD) or IC₅0. Competitive binding assays can also be performed using a labeled phosphopeptide tracer.
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| Cell Assay |
Cellular experiments for Caffeic acid-pYEEIE TFA are not standard, as the compound is primarily a biochemical reagent for studying SH2 domain interactions in cell-free systems. For cellular applications, the compound may need to be delivered via microinjection or conjugation to a cell-penetrating peptide. Readouts would include measuring the inhibition of Lck-dependent signaling events, such as phosphorylation of downstream substrates, using Western blot analysis.
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| Animal Protocol |
Detailed in vivo animal protocols for Caffeic acid-pYEEIE TFA are not described in the literature. Its application is strictly as a research tool for in vitro biochemistry. In vivo administration studies are not standard for this type of phosphopeptide inhibitor, and no specific dosing or animal model data are available from standard product documentation.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Caffeic acid-pYEEIE TFA are not applicable. As a phosphorylated or non-phosphorylated peptide (MW 1037.83), it is not designed for in vivo use. Its charged phosphate group (even in the non-phosphopeptide version, the scaffold contains a phosphonate-like moiety) and peptide backbone confer poor membrane permeability and susceptibility to phosphatase degradation in biological matrices. It is strictly an in vitro biochemical tool.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for Caffeic acid-pYEEIE TFA are not reported in standard product literature. As a research-use peptide inhibitor, standard safety assessments for acute toxicity, genotoxicity, and organ-specific toxicity are not typically described. For laboratory use, standard chemical safety precautions for handling peptides should be followed.
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| References | |
| Additional Infomation |
Caffeic acid-pYEEIE TFA has the molecular formula C41H₅1F3N₅O21P and a molecular weight of 1037.83. The CAS number is 507471-72-9. It appears as a white to off-white solid powder. The compound is stored at -20degC or -80degC, sealed, and away from moisture. It is soluble in water at 50 mg/mL and in DMSO. It exhibits 30-fold higher binding affinity for the src SH2 domain than Ac-pYEEIE. The product is for research use only.
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| Molecular Formula |
C41H51F3N5O21P
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| Molecular Weight |
1037.83
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| Related CAS # |
Caffeic acid-pYEEIE;507471-72-9
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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) |
H2O :~50 mg/mL (~48.18 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 | 0.9635 mL | 4.8177 mL | 9.6355 mL | |
| 5 mM | 0.1927 mL | 0.9635 mL | 1.9271 mL | |
| 10 mM | 0.0964 mL | 0.4818 mL | 0.9635 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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