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| 1mg |
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| Other Sizes |
| Targets |
PTBP1 alpha3-helix derived peptide P1 targets the RNA-binding domain of PTBP1, an important splicing factor. PTBP1 binds to RNA through its RNA recognition motifs (RRMs). This alpha3-helix peptide is derived from the alpha3-helix region of the PTBP1 protein and is a polypeptide that can inhibit RNA binding. It is a chemical probe for dissecting PTBP1-mediated alternative splicing regulation.
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| ln Vitro |
PTBP1 alpha3-helix derived peptide P1 is a polypeptide that inhibits RNA binding. As an alpha3-helix peptide derived from PTBP1, it is designed to disrupt the interaction between PTBP1 and its RNA targets, thereby inhibiting alternative splicing events regulated by PTBP1. The peptide is a useful tool for studying PTBP1 function in pre-mRNA splicing and RNA-protein interactions.
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| ln Vivo |
In vivo, PTBP1 alpha3-helix derived peptide P1 TFA can be used to study the functional roles of PTBP1 in cellular processes such as differentiation, oncogenesis, and neurological disorders. By inhibiting PTBP1-RNA binding, the peptide can modulate PTBP1-dependent alternative splicing, potentially affecting gene expression programs. It is primarily a chemical probe for dissecting PTBP1 biology in animal models.
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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 PTBP1 alpha3-helix derived peptide P1 TFA 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, and the IC50 for inhibition of RNA binding is calculated.
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| Cell Assay |
PTBP1 alpha3-helix derived peptide P1 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. After 24-48 hours, total RNA is extracted and reverse transcribed. RT-PCR is performed using primers flanking PTBP1-regulated exons. The ratio of spliced isoforms is analyzed by gel electrophoresis. PTBP1 protein levels are assessed by Western blot.
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| Animal Protocol |
PTBP1 alpha3-helix derived peptide P1 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 peptide (5-20 mg/kg, dissolved in PBS or 10% DMSO/PBS) daily. Tumor volume is measured every 2-3 days. PTBP1-dependent splicing changes in tumors are analyzed by RT-PCR.
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| ADME/Pharmacokinetics |
PTBP1 alpha3-helix derived peptide P1 TFA has a molecular formula of C63H110N26O20.xC2HF3O2, with a purity of ≥98%. The peptide has the sequence Ac-Asn-Gln-Ala-Arg-Ala-Gln-Ala-Ala-Leu-Gln-Ala-Val-Asn-Arg-NH2. The product appears as a white to off-white solid. It should be stored as a powder at -20degC. The TFA salt form ensures water solubility. Specific PK parameters have not been reported.
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| Toxicity/Toxicokinetics |
No detailed toxicity data are available for PTBP1 alpha3-helix derived peptide P1 TFA. As a research-grade peptide derived from an endogenous protein, it is expected to have low inherent toxicity. Standard safety precautions for peptide handling should be followed. Long-term safety and formal toxicology studies have not been conducted.
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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 alpha3-helix derived peptide P1 TFA is a research-grade peptide and is not approved for clinical use. It is a polypeptide that can inhibit RNA binding and is derived from the alpha3-helix region of PTBP1. This product is a chemical probe for studying PTBP1 function in RNA splicing and protein-RNA interactions. It is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C63H110N26O20.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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