| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH targets the Src SH2 domain with high affinity (IC50 = 0.5-1 µM). The phosphotyrosine residue at position 1 is critical for binding. It competitively inhibits the interaction between Src SH2 domain and native phosphotyrosine-containing ligands, thereby disrupting downstream signaling pathways.
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|---|---|
| ln Vitro |
In vitro, Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH binds with high affinity to the Src SH2 domain (IC50 = 0.5-1 µM). It blocks the binding of various SH2 domain constructs to platelet-derived growth factor kinase (IC50 = 1.35 µM). The peptide is used as a reference standard for SH2 domain binding studies.
|
| ln Vivo |
In vivo data for Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH are limited, as it is primarily used as an in vitro research tool. Cell-penetrating derivatives of similar phosphopeptides have been used in cell-based assays to disrupt SH2 domain-mediated signaling, but the unmodified peptide is not typically used in animal studies.
|
| Enzyme Assay |
For binding assays, recombinant GST-tagged Src SH2 domain (100-300 ng/well) is coated onto ELISA plates in PBS overnight at 4°C. After blocking with 2% BSA, biotinylated competitor phosphopeptide (4-10 nM) and increasing concentrations of Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH (0.001-100 µM) are added and incubated for 2 h at room temperature. Bound biotin is detected with streptavidin-HRP and TMB substrate.
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| Cell Assay |
For fluorescence polarization assays, FITC-labeled phosphopeptide probe (4-10 nM) is incubated with Src SH2 domain (50-150 nM) in assay buffer (20 mM HEPES, pH 7.5, 0.025% Triton X-100) for 30 min at room temperature. Increasing concentrations of Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH are added, and fluorescence polarization is measured. IC50 values are calculated from competition curves.
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| Animal Protocol |
For cell-based assays, if used, cells are treated with cell-penetrating derivatives of the phosphopeptide (10-100 µM) for 1-24 h. SH2 domain-dependent signaling (e.g., ERK phosphorylation, AKT activation) is assessed by Western blotting. Vehicle-treated cells serve as controls.
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| References |
| Molecular Weight |
803.704740000001
|
|---|---|
| Exact Mass |
803.262
|
| CAS # |
159439-02-8
|
| Related CAS # |
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA
|
| PubChem CID |
42628614
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| Sequence |
Ac--{Tyr(PO3H2)}-EEIE-OH
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| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.4±0.1 g/cm3
|
| Index of Refraction |
1.573
|
| LogP |
-2.73
|
| tPSA |
371.27
|
| Hydrogen Bond Donor Count |
11
|
| Hydrogen Bond Acceptor Count |
17
|
| Rotatable Bond Count |
25
|
| Heavy Atom Count |
55
|
| Complexity |
1450
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
CC[C@@H]([C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(C)=O)CC1=CC=C(OP(O)(O)=O)C=C1)=O)CCC(O)=O)=O)CCC(O)=O)=O)C(N[C@H](C(O)=O)CCC(O)=O)=O)C
|
| InChi Key |
QQEKQSBIEKQXQS-PSCZMIBCSA-N
|
| InChi Code |
InChI=1S/C32H46N5O17P/c1-4-16(2)27(31(48)36-22(32(49)50)11-14-26(43)44)37-29(46)21(10-13-25(41)42)34-28(45)20(9-12-24(39)40)35-30(47)23(33-17(3)38)15-18-5-7-19(8-6-18)54-55(51,52)53/h5-8,16,20-23,27H,4,9-15H2,1-3H3,(H,33,38)(H,34,45)(H,35,47)(H,36,48)(H,37,46)(H,39,40)(H,41,42)(H,43,44)(H,49,50)(H2,51,52,53)/t16-,20-,21-,22-,23-,27-/m0/s1
|
| Chemical Name |
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(4-phosphonooxyphenyl)propanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]pentanedioic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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) |
H2O
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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 | 1.2442 mL | 6.2212 mL | 12.4425 mL | |
| 5 mM | 0.2488 mL | 1.2442 mL | 2.4885 mL | |
| 10 mM | 0.1244 mL | 0.6221 mL | 1.2442 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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