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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
The molecular target of Tat-IKIP (46-60) is the IKK complex, specifically the protein-protein interaction interface between IKKbeta and NEMO. The IKIP-derived sequence is designed to mimic the binding motif that is crucial for the assembly and activation of the IKK complex. By competitively binding to this interface, the peptide prevents the formation of the active IKKbeta/NEMO complex, thereby blocking the phosphorylation and subsequent degradation of IkappaB. This, in turn, inhibits the nuclear translocation of the transcription factor NF-kappaB, preventing the expression of its pro-inflammatory target genes.
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| ln Vitro |
In vitro, Tat-IKIP (46-60) has been shown to potently suppress NF-kappaB activation. At a concentration of 5 uM, it significantly inhibits the LPS-induced phosphorylation of IKKalpha/beta and the nuclear translocation of the p65 subunit of NF-kappaB in mouse peritoneal macrophages. This inhibition translates into reduced production of pro-inflammatory cytokines. The Tat domain facilitates rapid cellular uptake, allowing the peptide to reach its intracellular target. It is not directly cytotoxic to cells at effective concentrations, making it a valuable tool for studying inflammatory pathways in vitro.
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| ln Vivo |
The in vivo efficacy of Tat-IKIP (46-60) has been validated in animal models of inflammatory diseases. It has been shown to significantly reduce DSS (dextran sulfate sodium)-induced acute inflammation in a mouse model of inflammatory bowel disease (IBD). Additionally, it attenuates zymosan-induced acute arthritis in an acute arthritis model (AAM). These effects are attributed to its ability to block NF-kappaB activation and suppress the downstream production of inflammatory cytokines. The Tat peptide ensures that the functional inhibitory sequence is delivered into cells in the target tissues in vivo.
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| Enzyme Assay |
General in vitro NF-kappaB activation assay (p65 Nuclear Translocation): Seed mouse peritoneal macrophages in 8-well chamber slides. Treat with Tat-IKIP (46-60) (0.1-10 uM) for 2 hours, then stimulate with LPS (100 ng/mL) for 30 minutes. Wash cells, fix, and permeabilize. Perform immunocytochemistry using an anti-NF-kappaB p65 antibody followed by a fluorescent secondary antibody. Cells are counterstained with DAPI to visualize nuclei. A significant reduction in the nuclear localization of p65 in the peptide-treated group compared to the LPS-only control is observed.
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| Cell Assay |
General in vitro cytokine production assay (ELISA): Seed mouse peritoneal macrophages in 96-well plates (1×10⁵ cells/well). Pre-treat with Tat-IKIP (46-60) (0.1-10 uM) for 1 hour, then stimulate with LPS (100 ng/mL) for 6 hours. Collect the cell culture supernatant and measure the concentration of TNF-alpha and IL-6 using a commercial ELISA kit. The peptide will significantly reduce the levels of these pro-inflammatory cytokines. For cytotoxicity, an MTT assay on parallel wells will show an IC50 > 50 uM.
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| Animal Protocol |
General in vivo animal protocol for inflammation efficacy: Dissolve Tat-IKIP (46-60) TFA in sterile water for injection or PBS. For the colitis model, administer DSS (3-5% in drinking water) to C57BL/6 mice (n=8/group) for 7 days to induce IBD. Mice are treated with the peptide (0, 5, 10, 20 mg/kg, i.p.) once daily starting from day 0. Mice are monitored daily for weight loss, stool consistency, and fecal bleeding. At the end of the study, colon length and histopathological score are assessed. The peptide will significantly reduce disease severity.
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| ADME/Pharmacokinetics |
As a synthetic peptide with a moderate molecular weight, Tat-IKIP (46-60) is likely rapidly cleared from the plasma after intraperitoneal (i.p.) administration. The TFA salt form is used to enhance solubility for in vivo injections. The Tat peptide facilitates rapid cellular uptake, but the peptide itself is short-lived in circulation (plasma half-life typically < 1 hour). It is likely metabolized by proteases into its constituent amino acids. For its use as a research standard, detailed PK/ADME profiles are not typically required.
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| Toxicity/Toxicokinetics |
Preclinical studies indicate that Tat-IKIP (46-60) is well-tolerated at therapeutic doses in mice, showing no overt signs of toxicity. As a small peptide, it is not considered genotoxic. It has not been evaluated in long-term carcinogenicity studies. For use as a research reference standard, it is handled as a standard laboratory chemical with typical safety precautions. Routine control at 0.15% is acceptable if it were to be present as an impurity, though it is typically a research compound.
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| References | |
| Additional Infomation |
Appearance: Lyophilized powder (as TFA salt). Molecular formula: (not disclosed). Storage: -20degC. Solubility: Soluble in water and PBS. Other names: Tat-Inhibitor of NF-kappaB Kinase-interacting Peptide (46-60), F1 peptide. Safety: For research use only.
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| Molecular Formula |
C145H246N48O31S.XC2HF3O2
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| Molecular Weight |
3189.87 (free base)
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| Related CAS # |
Tat-IKIP (46-60)
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| Sequence |
Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Leu-Leu-Ser-Leu-Ala-Met-Thr-Leu-Gly-Leu-Ala-Trp-Leu-Val-PheYGRKKRRQRRRLLSLAMTLGLAWLVF
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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, avoid exposure to moisture. |
| 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.
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