| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Wnt5a[1]
Box5 TFA directly targets the Wnt5a ligand, a key activator of the non-canonical Wnt signaling pathway. By binding to Wnt5a with high affinity, it acts as a competitive antagonist, preventing Wnt5a from interacting with its receptors, such as Frizzled (Fzd) and ROR1/2. This specific inhibition blocks the downstream signaling cascade, which includes the activation of Ca2+/calmodulin-dependent protein kinase II (CaMKII) and protein kinase C (PKC), as well as the suppression of the canonical beta-catenin pathway. |
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| ln Vitro |
In A2058 cells stimulated by rWnt5a (0.1 μg/mL), Box5 TFA (100 μM) decreases p-MARCKS expression [1].
In vitro, Box5 TFA (0.1 microg/mL) significantly inhibits recombinant Wnt5a (rWnt5a)-stimulated expression of p-MARCKS in A2058 melanoma cells. At a concentration of 100 microM, it effectively reduces the expression of p-MARCKS, a downstream effector of the non-canonical pathway. Furthermore, gene expression analysis has shown that Box5 prevents the expression of pro-apoptotic genes BAD and BAX, while increasing anti-apoptotic genes Bcl-xL, BCL2, and BCLW, indicating a neuroprotective effect. |
| ln Vivo |
In vivo, the specific activity of Box5 TFA has not been extensively detailed in the available literature. Research primarily focuses on its application as a tool compound for understanding Wnt5a biology in controlled laboratory settings. Further studies would be required to evaluate its pharmacokinetic properties and therapeutic potential in animal models of disease.
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| Enzyme Assay |
Non-cellular binding studies are typically performed using Surface Plasmon Resonance (SPR) or ELISA-based methods. The peptide is immobilized on a sensor chip or plate, and recombinant Wnt5a protein is flowed over the surface. Alternatively, a competitive binding assay can be conducted using labeled Box5 and increasing concentrations of unlabeled Wnt5a, or vice versa, to determine the binding affinity (KD) and specificity of the interaction.
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| Cell Assay |
Cellular assays to assess Box5 activity often utilize A2058 melanoma cells or N18D3 neuronal cells. Cells are serum-starved and pre-treated with Box5 TFA (e.g., 0.1-100 microM) before stimulation with recombinant Wnt5a (0.1 microg/mL). Following treatment, cell lysates are collected to assess the phosphorylation status of downstream effectors like MARCKS by Western blot. Cell migration is evaluated using transwell or wound-healing assays, and viability is assessed via MTT assays.
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| Animal Protocol |
In vivo animal experimental protocols for Box5 TFA are not standardly defined in the literature. The compound's role as a research tool means its use in animals would be specific to an investigator's hypothesis. A general protocol could involve administering Box5 TFA (e.g., via intraperitoneal or intratumoral injection) in a mouse xenograft model of melanoma to assess effects on tumor growth and metastasis.
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| ADME/Pharmacokinetics |
Dedicated pharmacokinetic (PK) studies for Box5 TFA are not available in standard literature. As a peptide-based antagonist, its systemic bioavailability is likely limited, and it would generally be considered unstable in serum unless modified. Comprehensive PK parameters such as half-life, volume of distribution, and clearance would need to be experimentally determined for its use as a therapeutic lead.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for Box5 TFA are not provided in standard product literature. As a research-use compound, standard safety assessments for acute toxicity, genotoxicity, and organ-specific toxicity are not typically described. For laboratory use, standard chemical safety precautions for handling peptides should be followed.
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| References | |
| Additional Infomation |
Box5 TFA has a molecular weight of 880.9 g/mol and a molecular formula of C32H51F3N6O15S2. It is typically stored as a powder at -20degC, protected from light and moisture. It shows promise as a research tool for melanoma and neuroprotection studies. This product is intended for research purposes only and is not for clinical use.
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| Molecular Formula |
C32H51F3N6O15S2
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| Molecular Weight |
880.90
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| Related CAS # |
Box5;1206604-29-6
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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) |
DMSO :~250 mg/mL (~283.80 mM)
H2O :~5 mg/mL (~5.68 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.26 mg/mL (3.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.6 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.36 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1352 mL | 5.6760 mL | 11.3520 mL | |
| 5 mM | 0.2270 mL | 1.1352 mL | 2.2704 mL | |
| 10 mM | 0.1135 mL | 0.5676 mL | 1.1352 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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