| Size | Price | Stock | Qty |
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| 5mg | |||
| 10mg | |||
| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Boc3Arg is a tert-butyl carbamate-protected arginine compound. It functions as an efficient tag to induce degradation by directly targeting proteins to the 20S proteasome. It does not have a specific receptor or enzyme target. The Boc3Arg moiety provides a general strategy for the design of degradation-inducing inhibitors. By chemically linking Boc3Arg to a protein or inhibitor, the tagged protein is recognized by the 20S proteasome and degraded without the need for a specific E3 ligase. This mechanism is distinct from PROTACs (which rely on E3 ligase recruitment). It is a chemical biology tool for studying protein function and degradation.
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| ln Vitro |
In vitro, Boc3Arg is an efficient tag for inducing protein degradation. The Boc3Arg moiety, when linked to a protein or inhibitor, directly localizes the target protein to the 20S proteasome, leading to its degradation. Boc3Arg provides a general strategy for the design of degradation-inducing inhibitors, with potential applications in chemical biology and drug discovery. It is a tert-butyl carbamate-protected arginine compound that can be conjugated to bioactive molecules via its carboxylic acid group.
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| ln Vivo |
In vivo, Boc3Arg is a chemical tag that can induce degradation of target proteins. Inhibitors linked to Boc3Arg induce selective degradation of their target proteins. The Boc3Arg moiety may provide a general strategy for constructing degradation-inducing inhibitors in vivo. Boc3Arg is a research-grade tag and is not a therapeutic agent. No specific in vivo data is provided.
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| Enzyme Assay |
The degradation activity of Boc3Arg can be assessed by Western blotting. Cells expressing the target protein are treated with a Boc3Arg-conjugated inhibitor (0.1-100 uM) for 4-24 h. The cells are lysed, and target protein levels are measured by Western blotting. The degradation is also assessed by incubating purified target protein with Boc3Arg in a cell-free 20S proteasome assay. The proteasome-dependent degradation is confirmed by using a proteasome inhibitor (e.g., MG132).
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| Cell Assay |
Not applicable. Boc3Arg is a chemical tag and is not used directly in cell-based assays for drug discovery. For degradation studies, cells are seeded in 6-well plates (3×10⁵ cells/well) and treated with a Boc3Arg-conjugated inhibitor (1-100 uM) for 4-24 h. Cell lysates are prepared, and target protein levels are assessed by Western blotting. DC₅0 (half-maximal degradation concentration) is calculated. Control treatments include vehicle alone and a proteasome inhibitor (MG132, 10 uM).
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| Animal Protocol |
In vivo degradation studies can be performed in mouse xenograft models. Boc3Arg is conjugated to a target-binding ligand (e.g., an inhibitor of an oncogenic protein). The conjugate is formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline and administered intraperitoneally (10-50 mg/kg) once daily for 1-2 weeks. Tumor tissues are harvested, and target protein levels are measured by Western blotting and immunohistochemistry. Boc3Arg-mediated degradation is expected to reduce target protein levels.
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| ADME/Pharmacokinetics |
Not applicable. Boc3Arg is a chemical tag, not a drug. It is not intended for systemic administration as a monotherapy. For research use, it is stored as a powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 6 months, -20degC for 1 month. It is soluble in DMSO (≥200 mg/mL, ~421.45 mM). The Boc3Arg moiety is stable under neutral and acidic conditions but can be cleaved by strong acids.
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| Toxicity/Toxicokinetics |
For Boc3Arg, hazard statements: H315 (Causes skin irritation), H319 (Causes serious eye irritation), H335 (May cause respiratory irritation). Signal word: Warning. Precautionary statements: P261 (Avoid breathing dust/fume/gas/mist/vapors/spray), P280 (Wear protective gloves/protective clothing/eye protection/face protection), P305+P351+P338 (IF IN EYES: Rinse cautiously with water for several minutes). Storage: at -20degC, sealed, protect from light.
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| References | |
| Additional Infomation |
Boc3Arg (Boc3-Arg) is a research-grade tert-butyl carbamate-protected arginine derivative used as a 20S proteasome-targeting tag for protein degradation. It is not an FDA-approved drug. It is used in chemical biology and drug discovery to induce targeted protein degradation, providing a PROTAC-alternative strategy. For research use only, not for diagnostic or therapeutic applications.
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| Molecular Formula |
C21H39N5O7
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|---|---|
| Molecular Weight |
473.56
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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 |
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1117 mL | 10.5583 mL | 21.1166 mL | |
| 5 mM | 0.4223 mL | 2.1117 mL | 4.2233 mL | |
| 10 mM | 0.2112 mL | 1.0558 mL | 2.1117 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.
Products are for research use only; We do not sell to patients
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