PeptideDB

PTD-p65-P1 Peptide

PTD-p65-P1 Peptide

CAS No.:

PTD-p65-P1 Peptide is a potent and specific inhibitor of the nuclear transcription factor NF-κB, derived from the p65 s
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PTD-p65-P1 Peptide is a potent and specific inhibitor of the nuclear transcription factor NF-κB, derived from the p65 subunit of NF-κB amino acid (AA) residues 271-282. It can selectively inhibit NF-κB induced by various inflammatory stimuli. κB activation downregulates NF-κB-mediated gene expression and upregulates apoptosis.

Physicochemical Properties


Molecular Formula C168H275N57O44S
Molecular Weight 3829.50
Related CAS # PTD-p65-P1 Peptide TFA
Appearance Typically exists as solid at room temperature
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

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets NF-kappaB[1]
ln Vitro PTD-p65-P1 Peptide (10-150 μM; 0-60 min; KBM-5 cells) reduces 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 (150 μM; 0–60 min; KBM-5 cells) prevents nuclear translocation and cytoplasmic p65 phosphorylation[1]. In KBM-5 cells, 100 μM of PTD-p65-P1 peptide potentiates TNF-induced apoptosis from 4 to 45%[1]. Inhibiting TNF-induced NF-κB-dependent reporter gene expression is PTD-p65-P1 Peptide (150 μM; A 293 cells) [1]. The PTD-p65-P1 Peptide (150 μM; 12-24 h; SP-53 cells) slows down the growth of cells [2].
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 Viability 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).
References

[1]. Identification of a p65 peptide that selectively inhibits NF-kappa B activation induced by various inflammatory stimuli and its role in down-regulation of NF-kappaB-mediated gene expression and up-regulation of apoptosis. J Biol Chem. 2004 Apr 9;279(15):15096-104.

[2]. Curcumin (diferuloylmethane) inhibits constitutive NF-kappaB activation, induces G1/S arrest, suppresses proliferation, and induces apoptosis in mantle cell lymphoma. Biochem Pharmacol. 2005 Sep 1;70(5):700-13.


Solubility Data


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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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).
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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.2611 mL 1.3057 mL 2.6113 mL
5 mM 0.0522 mL 0.2611 mL 0.5223 mL
10 mM 0.0261 mL 0.1306 mL 0.2611 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.