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PEGylation, the process of attaching Polyethylene Glycol (PEG) chains to molecules such as proteins, peptides, and antibody fragments, is a
Traditional PEGs, produced through polymerization, are heterogeneous mixtures that complicate characterization and application. In contrast, Precise PEG products are single molecules with defined lengths, molecular weights, and architectures, synthesized using our proprietary technology.
We offer a portfolio of over 6,000 high-purity PEG linkers, encompassing a diverse range of functional groups, including, but not limited to Azide, Amine, Alkyne, DBCO, BCN, TCO, Activated Ester, Maleimide, and Biotin.
In addition to our extensive inventory, we provide custom PEG linker synthesis services tailored to meet specific project requirements.
Antibody–Drug Conjugates (ADCs) are sophisticated therapeutic agents consisting of monoclonal antibodies covalently bound to cytotoxic drugs through chemical
With an inventory of over 1000 linker products, we support researchers with a broad array of high-quality options. Furthermore, our comprehensive customization services cater to diverse research objectives, enabling tailored solutions that align with the specific needs of each ADC project.
Click chemistry continues to gain popularity and is used in a variety of research fields with significant contributions to the
Copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC): CuAAC is a cornerstone of "click" chemistry, involving the reaction of azides with terminal alkynes in the presence of a copper(I) catalyst to form 1,2,3-triazoles. Renowned for its efficiency, selectivity, and versatility, CuAAC has broad applications across chemistry and biology. However, it is not without limitations; challenges include potential copper toxicity in biological systems and the difficulty of removing residual copper from final products. These issues are particularly significant in pharmaceutical and sensitive biomolecular applications, necessitating strategies to mitigate copper-related concerns.
Strain-promoted alkyne-azide cycloaddition (SPAAC): SPAAC has become a prominent bioorthogonal reaction, widely utilized in fields such as chemical biology, drug discovery, and materials science. This reaction stands out for its exceptional efficiency, speed, selectivity, and compatibility with living systems. Unlike other reactions, SPAAC does not require external stimuli such as light, heat, or catalysts. Its mechanism leverages the inherent strain energy of cyclic alkynes, which react readily with azides. Over time, diverse cyclooctyne derivatives have been engineered and optimized to enhance SPAAC reactivity and broaden its applications.
Inverse Electron Demand Diels–Alder (IEDDA) reaction: IEDDA is recognized for its unmatched kinetics, superior orthogonality, and biocompatibility, making it a standout among bioorthogonal reactions. An exemplary IEDDA reaction, known as TCO ligation and pioneered by Fox et al., entails the reaction of an electron-deficient tetrazine (Tz) with a strained trans-cyclooctene (TCO) derivative, making it an ideal tool for in vivo applications. Through collaborative licensing with Professor Fox's group, we are proud to offer a specialized selection of unique TCO and tetrazine compounds tailored to support your research needs.
The concurrent binding of a degrader molecule to two proteins—the protein of interest (POI) and an E3 ubiquitin
The design of effective PROTACs (proteolysis-targeting chimeras) demands precise control over linker length, shape, and attachment points to optimize binding affinity and functional efficacy. However, the heterobifunctional nature of PROTACs introduces considerable synthetic challenges, and computational tools often fall short in accurately predicting structure-activity relationships (SAR). Consequently, SAR exploration is primarily empirical, necessitating substantial investments of time and resources.
To address the challenges associated with PROTAC design and accelerate development, we have established a robust library of pre-formed E3-ligand linker intermediates. This resource enables the efficient synthesis of a wide array of diverse PROTAC candidates, facilitating their rapid evaluation and optimization for targeted protein degradation applications.
Acrylate PEG refers to a variant of polyethylene glycol characterized by homobifunctional or heterbifunctional acrylate end groups, affording it
The inclusion of the acrylate group facilitates radical or UV-initiated polymerization, along with thiol-ene reactions via Michael Addition. The acrylate functional group further enables the construction of polymers from the oligomeric polyethylene glycol monomer. Moreover, the acrylate functional end group of acrylate-substituted PEG can undergo reactions with thiol functional groups, such as those found in Cysteine residues, resulting in the formation of thioethers. By initially polymerizing these PEG compounds and subsequently combining the polymerized PEG compounds with proteins possessing thiol moieties, an effective immobilization of proteins onto surfaces can be achieved. Alternatively, proteins can be enclosed within a polymeric matrix, thereby offering additional versatility in applications.
Amino PEG, or PEG amine, constitutes a diverse class of compounds with notable synthetic significance. Distinguished by an amine
Aminooxy PEGs, also referred to as oxyamine PEGs, comprise a distinct category of polyethylene glycol compounds distinguished by aminooxy
Azido-functionalized PEG derivatives are increasingly finding applications in the realms of conjugation chemistry and targeted drug delivery. Their utility lies
The strain-promoted alkyne-azide cycloaddition (SPAAC) stands out as a widely adopted bioorthogonal reaction with extensive applications across diverse fields,
BCN PEG represents a click chemistry linker featuring a highly reactive BCN group at one end, coupled with polyethylene glycol. Among diverse cyclooctynes, BCN strikes a favorable balance between reactivity and hydrophilicity. Its exceptional reactivity, solubility, and chemoselectivity render it well-suited for applications in bioconjugations, labeling, and chemical biology in aqueous environments. BCN PEG serves as a valuable tool for imaging and tracking biomolecules, including proteins, lipids, and glycans, within their natural milieu.
Biotin PEG reagents represent a category of PEG linkers featuring a biotin moiety tethered to a PEG spacer, specifically
Bromo PEG stands as a derivative of polyethylene glycol characterized by a bromide group at one end and another
Noteworthy examples of Bromo PEG products include:
1. Bromo-PEG4-acid: A heterobifunctional, PEGylated crosslinker featuring a bromide and a carboxyl group at each end.
2. Bromo-PEG3-azide: A PEG-azide variant designed for copper-free click chemistry applications.
Bromoacetamide PEG, a PEG derivative featuring a bromoacetamide group, is a versatile reagent for the conjugation of
The strain-promoted alkyne-azide cycloaddition (SPAAC) has gained widespread adoption as a bioorthogonal reaction, finding extensive applications across diverse fields
DBCO PEG represents a specific category of PEG linker featuring a highly reactive DBCO (Dibenzocyclooctyne) group. DBCO exhibits the capability to react with azide groups without a catalyst through a strain-promoted click reaction. This reaction can be conducted either in an organic solvent or under mild buffer conditions and holds the advantage of not affecting other functional groups present in biological samples. DBCO is instrumental for bioconjugation in live cells, non-living samples, and whole organisms.
Exemplary DBCO PEG products include:
1. DBCO-PEG4-DBCO: A PEG linker characterized by two DBCO groups and a hydrophilic PEG spacer arm.
2. DBCO-PEG4-amido Mal: A bioorthogonal linker featuring azide and sulfhydryl reactivity, with distinct functional groups at each end.
Dinitrophenyl (DNP) serves as a hapten and stands among the early small molecules utilized to elicit specific and targeted
PrecisePEG presents a range of DNP PEG reagents featuring diverse active groups, including carboxylic acid, hydroxyl, azide, NHS ester, among others. The hydrophilic nature of the PEG linker facilitates an increased number of DNP groups to be conjugated to a biological molecule without inducing precipitation, thus enhancing the efficacy of bioconjugation processes.
DOTA PEG represents a distinct category of PEG linker featuring a DOTA (1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid) unit coupled with a
Applications of DOTA-PEG linkers encompass:
1. Development of targeted molecular imaging and therapy: Attaching the DOTA PEG linker to a targeting molecule, such as an antibody or a small molecule ligand, enables the selective delivery of therapeutic agents to specific cells or tissues in the body.
2. Advancements in novel therapeutics for cancer, neurological disorders, and inflammatory diseases: DOTA-PEG linkers play a pivotal role in enhancing the pharmacokinetic properties of drug conjugates, including increased half-life and reduced immunogenicity. These attributes contribute to the development of more effective and well-tolerated therapeutic interventions.
mPEG, or Methoxy PEG, stands as a polyethylene glycol (PEG) derivative with a reactive group at one end, while
Maleimide PEG, a subset of polyethylene glycol (PEG), features a maleimide group at one terminal end, serving as an
The expeditious and straightforward reaction between a thiol and a maleimide, leading to the formation of a thiosuccinimide product, has emerged as a preeminent method for site-selective modification of cysteine residues within the realm of bioconjugation technology. Within the pH range of 6.5 to 7.5, the thiol-maleimide reaction demonstrates chemoselectivity for thiols and engenders stable thioether bonds. It is noteworthy that beyond pH 7.5, free primary amines competitively react at the maleimide double bond. PEG Maleimide proves invaluable for bioconjugation and protein labeling endeavors, offering the capability to affix small molecules with PEG chains to proteins, peptides, or surfaces featuring sulfhydryl groups. This versatile application underscores the utility of Maleimide PEG in facilitating precise and controlled modifications in diverse biotechnological contexts.
PEG acids, constituting a subgroup within PEG compounds, are characterized by a carboxylic acid (COOH) group at one end and
PEG acid functionalities extend to the modification of biomolecules or surfaces featuring free amines, encompassing materials such as quantum dots, self-assembled monolayers, and magnetic particles. The applications of PEG acids span across diverse domains, including medical research, drug-release mechanisms, nanotechnology, new materials research, cell culture, as well as the synthesis of ligands and polypeptides. This versatility positions PEG acids as integral components in an array of scientific and technological advancements.
PEG Aldehyde constitutes a category of PEG derivatives featuring an aldehyde group at one terminus. This specialized PEG linker
Moreover, PEG Aldehyde finds application in bioconjugation endeavors by reacting its aldehyde group with aminooxy or hydrazide groups. The reversible nature of the conjugation is achieved by reacting with hydrazine or hydrazide groups, forming a hydrolytically labile acyl hydrazone linkage. This versatile functionality positions PEG Aldehyde as a pivotal tool for precise and controlled modifications in bioconjugation and pegylation strategies.
PEG CH2COOH acid represents a variant of PEG compound featuring a terminal carboxylic acid. Similar to the more common
PEG Hydrazide, a subset of PEG reagents, features a hydrazide functional group, enabling reactions with aldehydes, ketones, or carboxyl
The pH-sensitive nature of PEG hydrazone conjugates, coupled with controlled pH-sensitivity, holds promise for applications in biological stimuli-mediated drug targeting. Additionally, the hydrazide group exhibits reactivity with carbonyl groups, forming diacylhydrazide linkages, commonly employed in the PEGylation of glycosylated sites on proteins. Another notable application involves the creation of lipidated hydrazide PEG nanoparticles, characterized by self-assembling lipids encapsulating drugs, with hydrazide PEG contributing to enhanced stability, biocompatibility, and controlled drug release.
The utility of Hydrazide PEG reagents extends to drug research and development, featuring diverse applications in diagnostics and therapeutic protein modification, making them valuable tools in advancing pharmaceutical sciences.
PEG Mesylate is a PEG reagent distinguished by the presence of mesyl groups (methanesulfonyl, abbreviated as OMs) located at
In comparison to PEG Tosylate, PEG Mesylate exhibits higher reactivity but lower stability. Despite its reactivity, it remains soluble in water and polar organic solvents. PEG Mesylate finds diverse applications across the domains of chemistry, biochemistry, and materials science, playing a pivotal role in bioconjugation, drug delivery, polymer synthesis, and surface modification.
PEG NHS esters, a category of amine-reactive PEG reagents, are widely employed in the bioconjugation process with antibodies (ADC),
The reaction is conducted within the pH range of 7 to 9, with the optimal pH falling between 8.3 and 8.5. In this process, primary amines act as nucleophiles, attacking the NHS ester and releasing NHS as a byproduct. It is noteworthy that the NHS ester can undergo hydrolysis in aqueous solutions, which competes with the amine reaction and becomes more pronounced at higher pH levels.
Proteins, including antibodies, often feature multiple primary amines on their lysine (K) residues and N-termini of each polypeptide chain, making them suitable targets for PEG NHS ester labeling. This capability facilitates swift and straightforward surface modification of these biomolecules, presenting significant utility in applications such as targeted drug delivery.
PEG PFP esters, a subset of amine-reactive PEG reagents, are PEG derivatives featuring a pentafluorophenoyl (PFP) activated carboxylic acid
Similar to NHS esters, PEG PFP esters find widespread use in bioconjugation and the modification of biomolecules such as proteins, peptides, antibodies (ADC), and amine-modified oligonucleotides. Their rapid and facile capacity to modify the surfaces of these biomolecules is particularly valuable for applications in targeted drug delivery. Furthermore, PEG PFP esters can be employed to label the surfaces of nanoparticles and cells.
PEG Phosphonate represents a class of PEG derivatives in which a polyethylene glycol (PEG) chain is attached to a
PEG SDP ester is classified as an amine-reactive PEG reagent, featuring a sulfodichlorphenol (SDP) activated carboxylic group at one end
With superior stability in water and buffers, it excels in achieving high labeling yields under biologically relevant conditions, thereby enhancing control and consistency in conjugation reactions compared to other esters. The inclusion of the sulfo group on SDP significantly augments its water solubility, rendering it well-suited for physiological environments. PEG SDP ester finds extensive utility in the bioconjugation of proteins, peptides, antibodies (ADC), and various other molecules.
PEG sulfonic acid represents a class of polyethylene glycol (PEG) derivatives characterized by a sulfonic acid end group. These
PEG TFP ester is categorized as an amine-reactive PEG reagent, featuring a 2,3,5,6-tetrafluorophenol (TFP) functional group attached to one
In aqueous media, the optimal pH for conjugating TFP esters to amines surpasses that of NHS esters, with TFP esters favoring a range greater than 7.5, compared to the 7.0-7.2 range for NHS esters. However, it's noteworthy that TFP ester reagents exhibit lower water solubility than their NHS ester counterparts due to the hydrophobic nature of the TFP group on the PEG chain. This challenge can be addressed by employing water and water-miscible organic solvents, such as DMac or acetonitrile, to facilitate the reaction. In situations where organic solvents are restricted, NHS esters may be deemed more suitable than TFP esters.
PEG Tosylate is a PEG reagent characterized by the presence of tosyl groups at the terminus of the PEG
The inclusion of the PEG moiety in the molecule imparts solubility in both water and polar organic solvents, endowing hydrophilic properties to the modified compounds. PEG Tosylate finds diverse applications in the realms of chemistry, biochemistry, and materials science, playing a crucial role in bioconjugation, drug delivery, polymer synthesis, and surface modification.
SPDP PEG is a PEG reagent featuring a pyridyldithiol group at the end of the PEG chain. This particular group
Optimal conditions for the reaction between the pyridyldithiol group and sulfhydryl groups are achieved at pH 7-8 in a thiol-free buffer, with the subsequent release of pyridine-2-thione, quantifiable by its absorbance at 343 nm. The resultant disulfide-containing conjugates can be effectively reduced and cleaved by agents such as dithiothreitol (DTT), THPP, or TCEP. In most instances, a 25mM DTT solution at pH 4.5 proves sufficient to break the crosslinks without impacting the natural protein disulfides.
SPDP PEG is a PEG reagent featuring a pyridyldithiol group at the end of the PEG chain. This particular
Thiol PEG represents a polyethylene glycol (PEG) variant characterized by a sulfhydryl functional group at one terminus. This sulfhydryl
The utility of thiol PEG extends to the modification of surfaces across diverse materials, such as quantum dots, self-assembled monolayers, magnetic particles, and gold nanoparticles (AuNPs). By applying PEG chains to these surfaces, thiol PEG effectively mitigates non-specific protein binding, thereby enhancing biocompatibility and stability. Additionally, thiol PEG serves as a valuable reagent for the modification of proteins, peptides, and other biomolecules through the attachment of PEG chains.
Thiol PEG emerges as a versatile tool for surface and biomolecule functionalization, finding significant application in the realms of bionanotechnology and nanomedicine. Its diverse reactivity and compatibility make it a pivotal component in advancing these fields.
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