| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
PEGs
Desthiobiotin-PEG4-propargyl does not have a specific biological target itself but serves as a bioconjugation and affinity purification reagent. The desthiobiotin moiety binds reversibly to streptavidin, allowing for gentle elution of biotinylated molecules from streptavidin affinity columns. The propargyl (alkyne) group enables bioorthogonal click chemistry conjugation to azide-functionalized molecules. The PEG4 spacer provides water solubility and reduces steric hindrance during conjugation. |
|---|---|
| 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. The intracellular ubiquitin-proteasome system is utilized by PROTACs to specifically destroy target proteins[1].
In vitro studies demonstrate that Desthiobiotin-PEG4-propargyl functions as a bioconjugation and affinity purification reagent. The propargyl (alkyne) group allows for efficient conjugation to azide-containing molecules via CuAAc click reactions. The desthiobiotin moiety enables reversible binding to streptavidin, allowing for gentle elution under mild conditions. The PEG4 spacer provides water solubility and minimizes steric hindrance during conjugation. In vitro applications include labeling of biomolecules, affinity purification, and detection of azide-modified molecules. |
| ln Vivo |
In vivo activity data for Desthiobiotin-PEG4-propargyl as a standalone compound are not reported, as it is utilized as a bioconjugation and affinity purification reagent rather than as a therapeutic agent. The compound is designed for in vitro applications in protein labeling, affinity purification, and detection. Its in vivo applications would depend on the specific conjugated molecule and the overall properties of the complete bioconjugate.
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| Enzyme Assay |
In vitro assays for Desthiobiotin-PEG4-propargyl typically involve click conjugation studies to assess its reactivity with azide-containing molecules. The propargyl (alkyne) group can be conjugated to azide-functionalized molecules via CuAAc click reactions, and conjugation efficiency can be assessed by techniques such as mass spectrometry, HPLC, or gel electrophoresis. Streptavidin binding assays can be performed to evaluate the reversible binding of the desthiobiotin moiety to streptavidin. Elution efficiency can be assessed under various conditions.
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| Cell Assay |
In vitro cell-based assays using Desthiobiotin-PEG4-propargyl typically involve labeling of cellular components or biomolecules. Cells or cell lysates containing azide-modified biomolecules can be treated with Desthiobiotin-PEG4-propargyl via click chemistry for labeling and detection. The desthiobiotin moiety allows for subsequent affinity purification or detection using streptavidin-conjugated probes. Labeling efficiency and specificity can be assessed by Western blotting, fluorescence microscopy, or mass spectrometry.
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| Animal Protocol |
In vivo animal studies using Desthiobiotin-PEG4-propargyl are not typically performed, as the compound is primarily used as an in vitro bioconjugation and affinity purification reagent. The compound is intended for research use in labeling and purification applications.
|
| ADME/Pharmacokinetics |
As a bioconjugation reagent rather than a therapeutic drug, comprehensive pharmacokinetic data for Desthiobiotin-PEG4-propargyl alone are not available. The compound is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. The desthiobiotin moiety enables reversible streptavidin binding for affinity purification applications. The propargyl (alkyne) group enables click chemistry conjugation to azide-containing molecules.
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| Toxicity/Toxicokinetics |
The toxicity profile of Desthiobiotin-PEG4-propargyl as an individual compound is not extensively characterized, as it is primarily used as a research reagent. The compound is intended for research use only and is not approved for therapeutic use in humans. Standard laboratory safety practices, including the use of personal protective equipment and handling in a fume hood, are recommended.
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| References | |
| Additional Infomation |
Desthiobiotin-PEG4-propargyl (CAS 1951424-89-7) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. It is a click chemistry reagent containing an alkyne (propargyl) group that can undergo CuAAc with azide-containing molecules. The compound features desthiobiotin, a biotin analog that binds reversibly to streptavidin, allowing for gentle elution in purification workflows. It is part of the PEG category of PROTAC linkers and bioconjugation reagents.
|
| Molecular Formula |
C21H37N3O6
|
|---|---|
| Molecular Weight |
427.534986257553
|
| Exact Mass |
427.268
|
| CAS # |
1951424-89-7
|
| PubChem CID |
91757776
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| Appearance |
Light yellow to yellow viscous liquid
|
| LogP |
0
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
19
|
| Heavy Atom Count |
30
|
| Complexity |
522
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
O=C1N[C@@H](C)[C@@H](CCCCCC(NCCOCCOCCOCCOCC#C)=O)N1
|
| InChi Key |
CQSNBVBVAYQBHF-RBUKOAKNSA-N
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| InChi Code |
InChI=1S/C21H37N3O6/c1-3-10-27-12-14-29-16-17-30-15-13-28-11-9-22-20(25)8-6-4-5-7-19-18(2)23-21(26)24-19/h1,18-19H,4-17H2,2H3,(H,22,25)(H2,23,24,26)/t18-,19+/m0/s1
|
| Chemical Name |
6-[(4R,5S)-5-methyl-2-oxoimidazolidin-4-yl]-N-[2-[2-[2-(2-prop-2-ynoxyethoxy)ethoxy]ethoxy]ethyl]hexanamide
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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)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~233.9 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (5.85 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3390 mL | 11.6948 mL | 23.3896 mL | |
| 5 mM | 0.4678 mL | 2.3390 mL | 4.6779 mL | |
| 10 mM | 0.2339 mL | 1.1695 mL | 2.3390 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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