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| Targets |
PTBP1[1]
PTBP1-RNA-binding inhibitor P6 targets polypyrimidine tract-binding protein 1 (PTBP1), a key RNA-binding protein involved in pre-mRNA splicing regulation. PTBP1 binds to RNA through its RNA recognition motifs (RRMs). The stapled peptide P6 inhibits alternative splicing events regulated by PTBP1 by allosterically inhibiting PTBP1-RNA-binding, thereby disrupting the protein-RNA interaction. This mechanism allows for selective modulation of PTBP1-dependent splicing. |
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| ln Vitro |
In vitro, PTBP1-RNA-binding inhibitor P6 TFA is a stapled peptide inhibitor of the splicing factor PTBP1. It inhibits alternative splicing events regulated by PTBP1. The all-hydrocarbon staple stabilizes the alpha-helical conformation, which is critical for binding to PTBP1 and disrupting its RNA-binding function. The peptide is a valuable tool for studying post-transcriptional gene regulation and RNA-protein interactions.
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| ln Vivo |
In vivo, PTBP1-RNA-binding inhibitor P6 TFA can be used to study the functional roles of PTBP1 in cellular differentiation, oncogenesis, and neurological disorders. By inhibiting PTBP1-mediated alternative splicing, the peptide can modulate gene expression programs that are dependent on PTBP1. It has potential for therapeutic applications in diseases where PTBP1 dysregulation is implicated, such as cancer and neurodegenerative disorders.
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| Enzyme Assay |
A cell-free RNA-binding assay is used to measure PTBP1-RNA interaction. Purified PTBP1 protein (50-100 nM) is incubated with increasing concentrations (0.1-100 uM) of P6 peptide in binding buffer (20 mM HEPES pH 7.5, 150 mM KCl, 2 mM DTT). A fluorescently labeled RNA probe containing a PTBP1-binding site (e.g., a polypyrimidine tract) is added. Fluorescence polarization (FP) is measured. The IC50 for RNA-binding inhibition is calculated.
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| Cell Assay |
PTBP1-RNA-binding inhibitor P6 TFA is used in cell-based splicing assays. HeLa or HEK293 cells are seeded in 6-well plates. The peptide is delivered into cells using a cell-penetrating peptide fusion or by direct addition if the peptide is cell-permeable (the stapled peptide may have enhanced cellular uptake). After 24-48 hours, total RNA is extracted and reverse transcribed. RT-PCR is performed using primers flanking PTBP1-regulated exons (e.g., exon 10 of PKM gene). The ratio of spliced isoforms is analyzed by gel electrophoresis.
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| Animal Protocol |
PTBP1-RNA-binding inhibitor P6 TFA can be tested in mouse xenograft models of PTBP1-dependent cancers. Female BALB/c nude mice are implanted subcutaneously with cancer cells (e.g., glioblastoma or lung cancer cells). When tumors reach 100-150 mm3, mice are randomized and treated intraperitoneally with the P6 peptide (5-20 mg/kg, dissolved in PBS or 10% DMSO/PBS) daily for 14-21 days. Tumor volume is measured every 2-3 days. At the end of the study, tumors are excised, and PTBP1-dependent splicing changes are analyzed by RT-PCR.
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| ADME/Pharmacokinetics |
PTBP1-RNA-binding inhibitor P6 TFA is a stapled peptide with a molecular weight of approximately 1624 Da. The peptide has the sequence Ac-NQARAQAALQAVNR-NH2 with a stapled ring (Ala3-Ala7, Ala7-Ala11). The TFA salt ensures solubility. The product should be stored as a powder at -20degC. The all-hydrocarbon staple enhances peptide stability and cell permeability. Specific PK parameters have not been reported.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for PTBP1-RNA-binding inhibitor P6 TFA are available. As a research-grade peptide, it is used at low concentrations (uM range). Based on the roles of PTBP1 in normal cellular processes, prolonged or high-dose inhibition may cause adverse effects, but these have not been systematically studied. Standard safety precautions for peptide handling should be followed.
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| References |
[1]. Schmeing S, et al. Rationally designed stapled peptides allosterically inhibit PTBP1-RNA-binding. Chem Sci. 2023 Jul 13;14(31):8269-8278.
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| Additional Infomation |
PTBP1-RNA-binding inhibitor P6 TFA (PTBP1 alpha3-helix derived peptide P6 TFA) is a stapled peptide inhibitor of the splicing factor PTBP1. It inhibits alternative splicing events regulated by PTBP1 and is a valuable tool for studying RNA-protein interactions and the functional roles of PTBP1 in cellular differentiation, oncogenesis, and neurological disorders. This product is for research use only.
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| Molecular Formula |
C73H122N22O19.XC2HF3O2
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| Appearance |
Typically exists as solid at room temperature
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
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
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