| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
The primary targets of Maleimide-C10-NHS ester are primary amines and thiols on proteins, peptides, and other biomolecules. The NHS ester reacts with amines to form amide bonds, while the maleimide group reacts with thiols to form thioether bonds. The compound does not have a specific biological target but is used as a chemical tool for bioconjugation. These applications make it relevant for protein chemistry, drug delivery, and biosensor development.
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|---|---|
| ln Vitro |
One ligand is for an E3 ubiquitin ligase, and the other is for the target protein; these two ligands are joined by a linker to form PROTACs. To specifically destroy target proteins, PROTACs take advantage of the intracellular ubiquitin-proteasome system.[1]
In vitro, Maleimide-C10-NHS ester is used for the conjugation of proteins, peptides, and antibodies. The NHS ester reacts with primary amines under mild conditions (pH 7-9) to form stable amide bonds, while the maleimide group reacts with thiols (pH 6.5-7.5) to form stable thioether bonds. The 10-carbon spacer provides flexibility and distance. The compound is used in the preparation of protein conjugates, antibody-drug conjugates, and biosensors. These in vitro activities support its use in protein chemistry, drug delivery, and diagnostics. |
| ln Vivo |
In vivo, Maleimide-C10-NHS ester is not used as a therapeutic agent itself but is used in the preparation of conjugates for in vivo applications. Protein conjugates prepared using this compound have been used in drug delivery, imaging, and diagnostics. The compound’s reactivity with amines and thiols makes it useful for creating stable conjugates that can be administered in vivo. However, the compound itself is not administered systemically.
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| Enzyme Assay |
In vitro assays for Maleimide-C10-NHS ester involve testing its conjugation efficiency with model proteins or peptides. The compound is incubated with a protein (e.g., bovine serum albumin) at molar ratios ranging from 1:1 to 100:1 in buffered solutions (pH 7-8) for 1-24 hours. Conjugation efficiency is assessed by SDS-PAGE, MALDI-TOF, or HPLC. The reactivity of the NHS ester and maleimide groups is confirmed by the disappearance of the NHS peak and maleimide absorbance. All assays include appropriate controls.
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| Cell Assay |
In vitro cell-based assays for Maleimide-C10-NHS ester are not typically conducted with the compound itself. Instead, conjugates prepared using this compound are tested in cell-based assays to evaluate their biological activity. Cells are treated with conjugates at various concentrations, and the desired biological effect is measured. Cell viability is assessed using MTT assays. Experiments include vehicle controls and appropriate positive and negative controls.
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| Animal Protocol |
In vivo animal studies are not typically conducted with Maleimide-C10-NHS ester alone. Instead, conjugates prepared using this compound are evaluated in animal models. The conjugates are administered via intravenous or intraperitoneal injection at appropriate doses. Efficacy and pharmacokinetics are assessed. Each group consists of 6-10 animals with appropriate controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Maleimide-C10-NHS ester are not typically characterized, as it is a crosslinking reagent rather than a therapeutic agent. The compound is rapidly hydrolyzed in aqueous solution and reacts with amines and thiols to form stable conjugates. Its reactivity and stability in solution are characterized for bioconjugation applications.
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| References |
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
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| Additional Infomation |
Maleimide-C10-NHS ester is a heterobifunctional crosslinking reagent used for the conjugation of biomolecules through stable amide and thioether bonds. The 10-carbon spacer provides flexibility and distance between conjugated molecules. Widely used in protein chemistry, drug delivery, and biosensor development. Not approved for therapeutic use; intended for research purposes only.
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| Molecular Formula |
C₁₉H₂₆N₂O₆
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|---|---|
| Molecular Weight |
378.42
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| Exact Mass |
378.179
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| CAS # |
87981-04-2
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| PubChem CID |
5091658
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
520.4±42.0 °C at 760 mmHg
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| Flash Point |
268.5±27.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.552
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| LogP |
1.84
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
27
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| Complexity |
594
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N1C(C([H])=C([H])C1=O)=O)=O)N1C(C([H])([H])C([H])([H])C1=O)=O
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| InChi Key |
SGNVTRHWJGTNKV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H26N2O6/c22-15-10-11-16(23)20(15)14-8-6-4-2-1-3-5-7-9-19(26)27-21-17(24)12-13-18(21)25/h10-11H,1-9,12-14H2
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 11-(2,5-dioxopyrrol-1-yl)undecanoate
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| Synonyms |
MaleimideC10NHS ester; Maleimide C10 NHS ester
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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 | 2.6426 mL | 13.2128 mL | 26.4257 mL | |
| 5 mM | 0.5285 mL | 2.6426 mL | 5.2851 mL | |
| 10 mM | 0.2643 mL | 1.3213 mL | 2.6426 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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