| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
R18 TFA targets 14‑3‑3 proteins, a family of conserved regulatory molecules that bind to phosphorylated serine/threonine motifs in various signaling proteins. It competitively inhibits 14‑3‑3‑ligand interactions without requiring phosphorylation of the target protein. By blocking 14‑3‑3 binding to its ligands, R18 disrupts the ability of 14‑3‑3 to regulate the activity of its client proteins, including Raf‑1 kinase, Bad, ASK1, and exoenzyme S. This inhibition leads to the induction of apoptosis.
|
|---|---|
| ln Vitro |
In vitro, R18 TFA efficiently blocks the binding of 14‑3‑3 to the kinase Raf‑1, a physiological ligand of 14‑3‑3. It effectively abolishes the protective role of 14‑3‑3 against phosphatase‑induced inactivation of Raf‑1. The peptide induces apoptosis through its antagonistic activity on 14‑3‑3 proteins. Its Kd of 70‑90 nM confirms its high affinity for 14‑3‑3.
|
| ln Vivo |
Specific in vivo activity data for R18 TFA are not extensively detailed in available sources. As a peptide antagonist of 14‑3‑3 that induces apoptosis, it may have potential for in vivo studies in cancer models where 14‑3‑3 plays a role in cell survival and proliferation. However, detailed in vivo efficacy and pharmacokinetic data are not provided in the available literature.
|
| Enzyme Assay |
Non‑cellular binding assays for R18 TFA involve measuring its affinity for 14‑3‑3 proteins. These assays can be performed using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) with purified 14‑3‑3 protein. The peptide is incubated with 14‑3‑3, and the binding affinity (Kd) is determined from the resulting binding curves. Competition assays can also be performed to measure the peptide's ability to displace known 14‑3‑3 ligands.
|
| Cell Assay |
In vitro cellular assays for R18 TFA are performed using cells that express 14‑3‑3 and its client proteins. Cells are treated with the peptide, and the effects on 14‑3‑3‑ligand interactions, downstream signaling pathways, and apoptosis are assessed. The inhibition of Raf‑1 binding to 14‑3‑3 can be confirmed by co‑immunoprecipitation. Apoptosis induction is measured by caspase activation and other standard assays.
|
| Animal Protocol |
In vivo animal experiments for R18 TFA are not extensively detailed in available sources. As a peptide that induces apoptosis through 14‑3‑3 antagonism, it would typically be evaluated in tumor‑bearing mouse models. The compound would be administered via intraperitoneal or intravenous injection, and endpoints would include tumor growth inhibition, assessment of 14‑3‑3 target engagement, and evaluation of apoptosis markers in tumor tissues.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties for R18 TFA are not extensively detailed in available sources. The peptide has a molecular weight of 2309.7 and a molecular formula of C101H157N27O29S3. Its CAS number is 211364‑78‑2. The sequence is PHCVPRDLSWLDLEANMCLP (one‑letter code). It is a white lyophilized solid with a purity of >98% and is soluble in water. It should be stored under appropriate conditions for long‑term stability.
|
| Toxicity/Toxicokinetics |
Toxicological data for R18 TFA are not extensively detailed in available sources. As a peptide that induces apoptosis through 14‑3‑3 antagonism, it may have potential on‑target toxicities related to the disruption of 14‑3‑3‑mediated survival pathways. However, it is primarily used as a research tool and is not intended for human consumption. Comprehensive toxicological profiling would be required for any therapeutic development.
|
| References | |
| Additional Infomation |
R18 TFA is a bioactive peptide antagonist of 14‑3‑3 proteins with a Kd of 70‑90 nM. It competitively inhibits 14‑3‑3‑ligand interactions without requiring phosphorylation, blocking the binding of 14‑3‑3 to target proteins such as Raf‑1, Bad, ASK1, and exoenzyme S. It induces apoptosis and is used as a research tool for studying 14‑3‑3‑mediated signaling. It is not approved for clinical use and is intended for research purposes only.
|
| Molecular Formula |
C103H158F3N27O31S3
|
|---|---|
| Molecular Weight |
2423.73
|
| Related CAS # |
R18;211364-78-2
|
| Appearance |
White to off-white solid powder
|
| 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 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)
|
| Solubility (In Vitro) |
H2O :~50 mg/mL (~20.63 mM)
|
|---|---|
| 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 | 0.4126 mL | 2.0629 mL | 4.1259 mL | |
| 5 mM | 0.0825 mL | 0.4126 mL | 0.8252 mL | |
| 10 mM | 0.0413 mL | 0.2063 mL | 0.4126 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
