R18 TFA (Synonyms: PHCVPRDLSWLDLEANMCLP TFA) |
Catalog No.GC61601
One-Click Copy Product Info
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R18 TFA is a peptide antagonist of 14-3-3, with KD of 70-90nM.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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R18 TFA is a peptide antagonist of 14-3-3, with KD of 70-90nM [1]. R18 TFA can inhibit all members of the 14-3-3 protein family with a very similar affinity coefficient, and effectively utilize the amphiphilicity of the 14-3-3 binding channel to competitively inhibit phosphorylation and non-14-3-3-dependent protein-protein interactions [2]. Disruption of 14-3-3 via the R18 TFA switches nerve growth factor- and myelin-associated glycoprotein-dependent repulsion to attraction in rat DRG neurons [3]. The R18 TFA has been widely used to disrupt the binding of 14-3-3 to the ligands, thereby screening out the proteins that are regulated by 14-3-3[4].
In vitro, R18 TFA treatment at 8μM for 48 hours significantly inhibited the viability of MMQ cells and reduced the expression of 14-3-3η[5].
References:
[1] Wang B, Yang H, Liu Y C, et al. Isolation of high-affinity peptide antagonists of 14-3-3 proteins by phage display[J]. Biochemistry, 1999, 38(38): 12499-12504.
[2] Liu J, Cao S, Ding G, et al. The role of 14‐3‐3 proteins in cell signalling pathways and virus infection[J]. Journal of cellular and molecular medicine, 2021, 25(9): 4173-4182.
[3] Kent C B, Shimada T, Ferraro G B, et al. 14-3-3 proteins regulate protein kinase a activity to modulate growth cone turning responses[J]. Journal of Neuroscience, 2010, 30(42): 14059-14067.
[4] Repton C, Cullen C F, Costa M F A, et al. The phospho-docking protein 14-3-3 regulates microtubule-associated proteins in oocytes including the chromosomal passenger Borealin[J]. PLoS Genetics, 2022, 18(6): e1009995.
[5] Zhao S, Li B, Li C, et al. The apoptosis regulator 14-3-3η and its potential as a therapeutic target in pituitary oncocytoma[J]. Frontiers in endocrinology, 2019, 10: 797.
| Cell experiment [1]: | |
Cell lines | MMQ cells |
Preparation Method | MMQ cells were maintained in F12K medium supplemented with 2.5% fetal bovine serum (FBS) and 15% horse medium in humidified atmosphere with 5% CO2 at 37°C. Cells were seeded in 96-well plates at a density of 1×104 cells per well. After 24h, cells were incubated in the presence of 8μM R18 TFA, or the vehicle alone (DMSO) for 48h. Cell proliferation was measured. |
Reaction Conditions | 8μM; 48h |
Applications | R18 TFA treatment inhibited the cell viability of MMQ cells. |
References: | |
| Cas No. | SDF | ||
| Synonyms | PHCVPRDLSWLDLEANMCLP TFA | ||
| Formula | C103H158F3N27O31S3 | M.Wt | 2423.73 |
| Solubility | Water : < 0.1 mg/mL (ultrasonic) (insoluble) | Storage | -80°C, away from moisture |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 412.6 μL | 2.0629 mL | 4.1259 mL |
| 5 mM | 82.5 μL | 412.6 μL | 825.2 μL |
| 10 mM | 41.3 μL | 206.3 μL | 412.6 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)