| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
14-3-3 protein[1]
14-3-3 protein, which binds to phosphorylated serine/threonine motifs on target proteins and regulates their localization, activity, and stability. |
|---|---|
| ln Vitro |
Difopein competitively binds to 14-3-3 with high affinity, blocking the ability of 14-3-3 to interact with its ligand partners; it induces apoptosis and enhances the cytotoxic activity of cisplatin in cancer cells.
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| ln Vivo |
No in vivo activity data are available for this specific peptide; as a 14-3-3 inhibitor, it may promote apoptosis and sensitize tumors to chemotherapy in animal models, but detailed in vivo studies are lacking.
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| Enzyme Assay |
The 14-3-3 binding assay is performed by incubating recombinant 14-3-3 protein with biotinylated phosphopeptide ligands in the presence of increasing Difopein concentrations; bound complexes are captured on streptavidin-coated plates and detected with anti-14-3-3 antibody.
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| Cell Assay |
Cancer cells (e.g., HeLa, MCF-7) are treated with 1-50 microM Difopein for 24-72 hours; apoptosis is assessed by Annexin V/PI staining, caspase-3 activation, and PARP cleavage; combination treatment with cisplatin determines chemosensitization.
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| Animal Protocol |
No standardized animal protocol exists for Difopein; a typical efficacy study would involve subcutaneous tumor xenografts in mice treated intratumorally or systemically with Difopein, alone or with cisplatin, monitoring tumor volume and survival.
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| ADME/Pharmacokinetics |
PK properties for Difopein TFA are not reported; as a peptide, it may have poor oral bioavailability and short plasma half-life due to proteolytic degradation.
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| Toxicity/Toxicokinetics |
No dedicated toxicity studies for Difopein are available; however, as a peptide that inhibits 14-3-3 (a ubiquitous regulatory protein), off-target effects and broad cellular impact are potential concerns.
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| References | |
| Additional Infomation |
Difopein is a research tool for studying 14-3-3 biology; it has not entered clinical trials or received marketing approval for any therapeutic indication.
|
| Molecular Formula |
C275H425N76F3O91S6
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|---|---|
| Molecular Weight |
6501.19
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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 :~25 mg/mL (~3.85 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 | 0.1538 mL | 0.7691 mL | 1.5382 mL | |
| 5 mM | 0.0308 mL | 0.1538 mL | 0.3076 mL | |
| 10 mM | 0.0154 mL | 0.0769 mL | 0.1538 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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