| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
EMCS Crosslinker does not have a biological target in the traditional sense; it is a chemical reagent for bioconjugation. Its "targets" are functional groups on biomolecules: the NHS ester reacts with primary amines (-NH₂) on proteins, peptides, or other molecules, forming stable amide bonds; the maleimide group reacts with sulfhydryl groups (-SH) on cysteine residues, forming stable thioether bonds. This heterobifunctional nature allows for the conjugation of two different molecules.
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| ln Vitro |
The peptide was connected to the 6-maleimidocaproate N-hydroxysuccinimide ester, which was subsequently attached to an adenovirus vector carrying a luciferase gene [1].
EMCS itself is not a biologically active compound with inhibitory or stimulatory effects. Its utility lies in its chemical reactivity, enabling the creation of bioconjugates for various applications. Unlike zero-length crosslinkers (EDC/NHS), EMCS allows for controlled, two-step conjugation, which is critical when linking two macromolecules. It is a non-cleavable crosslinker, resulting in stable conjugates. |
| ln Vivo |
EMCS has no inherent in vivo biological activity as it is a chemical reagent. Its utility in vivo depends on the bioconjugates created using it. For example, EMCS can be used to conjugate antibodies to drugs or toxins for targeted therapy (ADCs). The resulting conjugates can be administered to animals for studying targeted delivery, biodistribution, and efficacy. The EMCS crosslinker itself is not administered as a therapeutic agent.
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| Enzyme Assay |
There are no enzyme/receptor binding assays for EMCS as it is not a drug targeting a biological receptor. However, the compound's reactivity with amines and thiols can be assessed in vitro by incubating it with amine- or thiol-containing molecules and analyzing conjugation efficiency using mass spectrometry, SDS-PAGE, HPLC, or ELISA. The formation of stable amide and thioether bonds confirms successful conjugation.
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| Cell Assay |
Cellular assays for EMCS involve labeling cell surface proteins. Cells are treated with EMCS (or a pre-formed conjugate containing EMCS) and incubated under appropriate conditions. Labeling efficiency is assessed by flow cytometry, fluorescence microscopy, or Western blotting using detection reagents specific to the conjugated molecule. Cell viability assays are performed to assess cytotoxicity of the conjugate.
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| Animal Protocol |
In vivo animal studies using EMCS are typically conducted with bioconjugates prepared using EMCS, such as antibody-drug conjugates or immunoconjugates. The conjugate is administered to animals (e.g., mice) via intravenous injection. Biodistribution, tumor targeting, efficacy, and toxicity are assessed. The EMCS crosslinker itself is not administered as a free compound in these studies. The stability of the conjugate in vivo is evaluated.
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| ADME/Pharmacokinetics |
EMCS has molecular weight of 308.29 g/mol (C₁₄H₁₆N₂O₆). It is soluble in DMSO at up to 230 mg/mL. The compound is typically stored at -20°C, protected from moisture and light. As a chemical crosslinker, pharmacokinetic studies are not typically performed for EMCS itself, as it is not administered as a therapeutic agent. Once conjugated to proteins, the resulting conjugates have their own PK properties.
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| Toxicity/Toxicokinetics |
EMCS is a chemical reagent and is not intended for human therapeutic use. Standard laboratory safety precautions should be followed when handling EMCS to avoid inhalation, ingestion, and skin contact. The compound is moisture-sensitive and should be stored properly. No systemic toxicity data is available as it is not intended for in vivo administration as a free compound. The NHS ester can react with amine groups on proteins, potentially causing irritation.
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| References |
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| Additional Infomation |
EMCS (6-Maleimidohexanoic acid N-hydroxysuccinimide ester) is a heterobifunctional crosslinker with an amine-reactive NHS ester and a sulfhydryl-reactive maleimide group. It is used for preparing hapten conjugates, enzyme immunoconjugates, and ADCs. It allows for controlled, two-step conjugation. It is a research reagent, not a therapeutic agent.
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| Molecular Formula |
C14H16N2O6
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|---|---|
| Molecular Weight |
308.2866
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| Exact Mass |
308.1
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| CAS # |
55750-63-5
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| PubChem CID |
5091655
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
480.6±47.0 °C at 760 mmHg
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| Melting Point |
70-73 °C(lit.)
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| Flash Point |
244.5±29.3 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.577
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| LogP |
-0.81
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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 |
8
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| Heavy Atom Count |
22
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| Complexity |
520
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VLARLSIGSPVYHX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H16N2O6/c17-10-5-6-11(18)15(10)9-3-1-2-4-14(21)22-16-12(19)7-8-13(16)20/h5-6H,1-4,7-9H2
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 6-(2,5-dioxopyrrol-1-yl)hexanoate
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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 : ~230 mg/mL (~746.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (24.33 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 75.0 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: ≥ 7.5 mg/mL (24.33 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 75.0 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: ≥ 7.5 mg/mL (24.33 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 | 3.2437 mL | 16.2185 mL | 32.4370 mL | |
| 5 mM | 0.6487 mL | 3.2437 mL | 6.4874 mL | |
| 10 mM | 0.3244 mL | 1.6218 mL | 3.2437 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.