| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
GMBS crosslinker targets primary amines (via NHS ester) and sulfhydryl groups (via maleimide) on proteins. It is used for chemical crosslinking of proteins as well as crosslinking mass spectrometry (CXMS) to study protein folding and map interfaces between interacting proteins. In ADC development, it links antibodies to payload molecules.
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|---|---|
| ln Vitro |
In vitro, GMBS is used for chemical crosslinking of proteins via their amine and thiol groups, leading to the formation of stable protein conjugates. It is commonly utilized in chemical crosslinking of proteins coupled with mass spectrometry to investigate protein folding and interactions. The compound is also used for peptide and antibody conjugation.
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| ln Vivo |
GMBS is not typically used as a therapeutic agent in vivo; rather, it is a research tool for protein crosslinking. However, its derivatives and conjugates may be used in vivo for ADC applications. As a non-cleavable linker, GMBS-based ADCs are designed for targeted drug delivery.
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| Enzyme Assay |
For protein crosslinking, GMBS is dissolved in an appropriate buffer (e.g., PBS or HEPES, pH 7.2-7.5) at a concentration of 1-10 mM. The protein of interest is incubated with GMBS at a molar ratio of 1:5 to 1:50 for 30-120 minutes at room temperature or 4°C. The reaction is quenched by adding excess Tris or glycine. Crosslinked products are analyzed by SDS-PAGE or mass spectrometry.
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| Cell Assay |
Cells expressing target proteins are lysed and incubated with GMBS for crosslinking. Alternatively, live cells are treated with membrane-permeable or impermeable crosslinkers depending on the study design. Crosslinked protein complexes are immunoprecipitated or purified and analyzed by Western blot or mass spectrometry to identify protein-protein interactions.
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| Animal Protocol |
For in vivo crosslinking studies, GMBS or GMBS-conjugated molecules are administered to animals via intravenous injection or other routes. Tissues are collected, and crosslinked protein complexes are analyzed. However, GMBS itself is primarily a research tool for in vitro protein crosslinking rather than a therapeutic agent for in vivo administration.
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| ADME/Pharmacokinetics |
GMBS has molecular formula C₁₂H₁₂N₂O₆, molecular weight 280.23. It is soluble in DMSO (~50 mg/mL, ~178.42 mM). The compound has density 1.5±0.1 g/cm³, boiling point 461.3±47.0°C at 760 mmHg, melting point 123-129°C, and LogP -1.56. It is a heterobifunctional crosslinker for amine-to-thiol conjugation.
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| Additional Infomation |
GMBS is a non-cleavable heterobifunctional crosslinker widely used in ADC development and protein crosslinking research. It contains an NHS ester that reacts with primary amines and a maleimide group that reacts with sulfhydryl groups. The short spacer arm of 7.3 Å makes it suitable for studying close protein-protein interactions. It is commonly used in crosslinking mass spectrometry (CXMS) to study protein folding and map interfaces between interacting proteins.
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| Molecular Formula |
C12H12N2O6
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|---|---|
| Molecular Weight |
280.23348
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| Exact Mass |
280.069
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| CAS # |
80307-12-6
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| PubChem CID |
133440
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
461.3±47.0 °C at 760 mmHg
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| Melting Point |
123-129ºC
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| Flash Point |
232.8±29.3 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.595
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| LogP |
-1.56
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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 |
6
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| Heavy Atom Count |
20
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| Complexity |
490
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1N(CCCC(ON2C(=O)CCC2=O)=O)C(=O)C=C1
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| InChi Key |
PVGATNRYUYNBHO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H12N2O6/c15-8-3-4-9(16)13(8)7-1-2-12(19)20-14-10(17)5-6-11(14)18/h3-4H,1-2,5-7H2
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 4-(2,5-dioxopyrrol-1-yl)butanoate
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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) |
DMSO : ~50 mg/mL (~178.42 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.92 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 25.0 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: ≥ 2.5 mg/mL (8.92 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 25.0 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: ≥ 2.5 mg/mL (8.92 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 | 3.5685 mL | 17.8425 mL | 35.6850 mL | |
| 5 mM | 0.7137 mL | 3.5685 mL | 7.1370 mL | |
| 10 mM | 0.3568 mL | 1.7842 mL | 3.5685 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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