| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
NF-kappaB[1]
PTD-p65-P1 targets the p65 subunit of NF-kappaB (nuclear factor kappa-light-chain-enhancer of activated B cells). The peptide is derived from the p65 subunit amino acid residues 271-282. It selectively inhibits NF-kappaB activation induced by various inflammatory stimuli by interfering with p65 nuclear translocation and cytoplasmic p65 phosphorylation. The PTD sequence enables the peptide to cross cell membranes and reach its intracellular target. |
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| ln Vitro |
PTD-p65-P1 Peptide TFA (10-150 μM; 0-60 min; KBM-5 cells) suppresses TNF-induced NF-κB activation by 25% at 100 μM and totally at 150 μM[1]. It also inhibits TNF-induced NF-κB activation in a dose-dependent manner. PTD-p65-P1 Peptide TFA (150 μM; 0–60 min; KBM-5 cells) prevents nuclear translocation and cytoplasmic p65 phosphorylation[1]. TNF-induced apoptosis is potentiated from 4 to 45% in KBM-5 cells when exposed to 100 μM of PTD-p65-P1 Peptide TFA for 16 hours[1]. In A 293 cells, PTD-p65-P1 Peptide TFA (150 μM) suppresses TNF-induced NF-κB-dependent reporter gene expression[1]. SP-53 cells treated with 150 μM PTD-p65-P1 Peptide TFA for 12-24 hours suppresses cell proliferation[2].
In vitro, PTD-p65-P1 Peptide TFA at 10-150 microM for 0-60 min in KBM-5 cells reduces TNF-induced NF-kappaB activation by 25% at 100 microM and completely at 150 microM. At 150 microM for 0-60 min, it prevents nuclear translocation and cytoplasmic p65 phosphorylation. TNF-induced apoptosis is potentiated from 4 to 45% in KBM-5 cells when exposed to 100 microM for 16 hours. The peptide down-regulates NF-kappaB-mediated gene expression. |
| ln Vivo |
In vivo, PTD-p65-P1 Peptide TFA can be used to study NF-kappaB inhibition and its effects on inflammation, cancer, and apoptosis. By inhibiting NF-kappaB activation, the peptide down-regulates NF-kappaB-mediated gene expression and up-regulates apoptosis. It is a cell-permeable NF-kappaB inhibitor, making it suitable for systemic administration in animal models of inflammatory diseases and cancer.
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| Enzyme Assay |
A cell-free binding assay for PTD-p65-P1 is not typical. The compound inhibits NF-kappaB by preventing p65 nuclear translocation and cytoplasmic phosphorylation, which requires cellular context. To assess p65 binding, an electrophoretic mobility shift assay (EMSA) can be performed using nuclear extracts from treated cells and a 32P-labeled NF-kappaB consensus DNA probe. The decrease in shifted complex indicates inhibition of NF-kappaB DNA binding.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: KBM-5 cells Tested Concentrations: 150 μM Incubation Duration: 0, 5, 10, 15, 30 and 60 minutes Experimental Results: Suppressed TNF-induced NF-κB activation by inhibiting phosphorylation and nuclear translocation of p65. Cell Proliferation Assay[2] Cell Types: SP-53 cells Tested Concentrations: 150 μM Incubation Duration: 12 and 24 hrs (hours) Experimental Results: Inhibited cell proliferation of 40% in 12 hrs (hours) and 60% in 24 hrs (hours). KBM-5 cells (human chronic myelogenous leukemia cells) are seeded in 6-well plates in RPMI-1640 + 10% FBS. Cells are treated with PTD-p65-P1 Peptide TFA (10-150 microM) for 0-60 min, followed by stimulation with TNF-alpha (10 ng/mL) for 30 min. Nuclear and cytoplasmic extracts are prepared. NF-kappaB activation is assessed by EMSA. p65 nuclear translocation is analyzed by Western blot of nuclear extracts. Cytoplasmic p65 phosphorylation is assessed by Western blot with anti-phospho-p65 antibody. Apoptosis is measured by Annexin V/PI staining. |
| Animal Protocol |
PTD-p65-P1 Peptide TFA can be tested in mouse models of inflammation, such as LPS-induced septic shock or colitis. BALB/c mice (20-25 g, n=8-10 per group) are injected intraperitoneally (i.p.) with LPS (10 mg/kg). PTD-p65-P1 Peptide TFA (1-5 mg/kg, dissolved in PBS) is administered i.p. 30 min before LPS. Serum levels of TNF-alpha, IL-6, and IL-1beta are measured by ELISA. Lung and liver tissues are collected for MPO activity and H&E staining. Survival is monitored. PTD-p65-P1 Peptide TFA also up-regulates apoptosis, which can be measured by TUNEL.
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| ADME/Pharmacokinetics |
PTD-p65-P1 Peptide TFA is a cell-permeable peptide that selectively inhibits NF-kappaB activation. Specific PK parameters (t½, Cmax, AUC) have not been reported. As a peptide, its plasma half-life is expected to be short (<30 min). The PTD sequence enhances cellular uptake but does not significantly stabilize the peptide against proteolytic degradation. The TFA salt enhances solubility. For in vivo use, the compound can be dissolved in PBS or sterile saline.
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| Toxicity/Toxicokinetics |
No detailed toxicity data are available for PTD-p65-P1 Peptide TFA. In animal studies, the compound was well-tolerated at the doses used (1-5 mg/kg i.p.). As an NF-kappaB inhibitor, the primary safety concern is immunosuppression and increased susceptibility to infections. No overt signs of systemic toxicity have been reported. Standard safety precautions for peptide handling should be followed.
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| References |
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| Additional Infomation |
PTD-p65-P1 Peptide TFA is a research-grade peptide and is not approved for clinical use. It is a potent, selective nuclear transcription factor NF-kappaB inhibitor derived from the p65 subunit of NF-kappaB. The PTD sequence allows the peptide to cross cell membranes, making it a useful tool for intracellular NF-kappaB inhibition in both in vitro and in vivo studies. This product is for research use only.
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| Molecular Formula |
C170H276F3N57O46S
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| Molecular Weight |
3943.52
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| Related CAS # |
PTD-p65-P1 Peptide
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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 (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) |
H2O :≥ 100 mg/mL (~25.36 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 | 0.2536 mL | 1.2679 mL | 2.5358 mL | |
| 5 mM | 0.0507 mL | 0.2536 mL | 0.5072 mL | |
| 10 mM | 0.0254 mL | 0.1268 mL | 0.2536 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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