| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PEGs
Mal-PEG10-NHSester does not target biological receptors; it serves as a chemical linker in PROTAC synthesis. In PROTACs, one end (malemide or NHS ester) links to a ligand for an E3 ubiquitin ligase, while the other end attaches to a ligand for a target protein, facilitating targeted protein degradation via the ubiquitin-proteasome system. |
|---|---|
| ln Vitro |
A linker separates the two ligands that make up PROTACs; one ligand is for an E3 ubiquitin ligase, and the other is for the target protein. Target proteins are selectively degraded by PROTACs by taking advantage of the intracellular ubiquitin-proteasome system[1].
Not available. As a PROTAC linker, its in vitro activity is assessed when incorporated into a complete PROTAC molecule. The PEG10 spacer provides optimal distance between target-binding and E3 ligase-binding moieties. Linker length and composition critically influence PROTAC ternary complex formation and degradation efficacy. |
| ln Vivo |
Not available. PROTACs containing PEG10-based linkers have demonstrated in vivo efficacy in degrading target proteins and inducing anti-tumor effects in mouse xenograft models. The PEG spacer improves solubility and pharmacokinetic properties, with activity typically assessed by target protein knockdown measured by Western blot of tumor tissues.
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| Enzyme Assay |
Not available. Standard NHS ester reactivity assays involve incubating Mal-PEG10-NHSester (1-100 uM) with amine-containing molecules (e.g., lysine or amino-PEG derivatives) in PBS buffer (pH 7.4) at room temperature for 1-2 hours, followed by HPLC-MS analysis to confirm conjugation efficiency. Maleimide-thiol conjugation is assessed by similar methods with DTT-reduced thiols.
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| Cell Assay |
Not available. For PROTAC activity assays, typical protocols involve treating target-expressing cells (e.g., cancer cell lines) with PROTACs synthesized using Mal-PEG10-NHSester (0.001-10 uM) for 4-24 hours, followed by Western blotting to quantify target protein degradation. PEG10 linkers generally exhibit low cellular toxicity as they are not pharmacologically active alone.
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| Animal Protocol |
Not available. For in vivo studies of PROTACs containing PEG10 linkers, standard protocols involve intravenous or intraperitoneal administration (typically 10-100 mg/kg) in tumor-bearing mice, with target protein levels assessed in tumor and normal tissues by Western blot at 4-24 hours post-dose. Efficacy is monitored by tumor volume change over 2-4 weeks.
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| ADME/Pharmacokinetics |
The PEG10 spacer improves aqueous solubility and reduces aggregation compared to shorter or hydrophobic linkers. The NHS ester is reactive with primary amines (pH 7-9), with a hydrolysis half-life of 1-4 hours in aqueous buffer. The maleimide group reacts with thiols (pH 6.5-7.5) with a half-life of minutes to hours.
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| Toxicity/Toxicokinetics |
The NHS ester is an irritant and may cause sensitization. The maleimide group can be toxic if not properly quenched. Mal-PEG10-NHSester is not intended for in vivo use as a free compound, as it is highly reactive. Specific toxicological studies have not been reported for this linker.
|
| References |
[1]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-991.
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| Additional Infomation |
Mal-PEG10-NHSester is a research-grade PROTAC linker for synthesizing targeted protein degraders. It has not entered clinical trials nor been approved for therapeutic use. The TFA salt of related compounds may be available, but this product is generally provided as the NHS ester form. This compound is strictly for laboratory research in protein degradation and chemical biology.
|
| Molecular Formula |
C31H50N2O16
|
|---|---|
| Appearance |
Colorless to light yellow oil
|
| SMILES |
O=C1C=CC(N1CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(ON2C(CCC2=O)=O)=O)=O
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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)
|
| Solubility (In Vitro) |
DMSO :~100 mg/mL (~141.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.54 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 (3.54 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 (3.54 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.) |
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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