-S-S- Cleavable Linkers

Recently, -S-S- reduction sensitive nanoparticles have attracted a lot of interest to address the problem of fast drug release in cells. Such nanoparticles typically consist of a drug-loaded core and a hydrophilic shell, introducing disulfide bonds into the carrier backbone, side chains, or crosslinkers. Disulfide bond can exist stably outside the cell, but when the nanoparticles enter into the tumor cells, they can exchange disulfide bond with the high concentration of glutathione (GSH) in the cytoplasm, resulting in the disulfide bond breaking and the destruction of the carrier structure, so as to achieve the purpose of rapid drug release. Disulfide bond breakage can occur not only in the cytoplasm, but also in lysosomes, due to the presence of gamma-interferon-induced lysosomal mercaptan (GILT), which can reduce disulfide bonds.

CD Bioparticles' services with customized delivery strategies, precise designs and modifications of drugs or drug-contained cargos, and advanced technical platforms can help you to solve:

The challenges you might meet:

• The efficacy and safety of the drug delivery system are inadequate
• The aggregation rate of loaded drugs at the tumor site is low
• Antitumor drugs are difficult to release effectively at focal sites
• Drugs have a shorter circulation time in the blood
• Drugs cannot penetrate deep into tumor tissue to reach tumor cells
• Intracellular drug release is difficult to achieve
• The drug carrier itself is highly toxic
• The linker is unstable in blood circulation and has more side effects
• Complex -S-S- cleavable linkers are difficult to synthesize
• Cleavable linkers cannot break under mild conditions

Key features:

• 2-hydroxyethyl disulfide mono-Tosylate
• Acid-PEG2-SS-PEG2-acid
• Acid-PEG3-SS-PEG3-acid
• Acid-PEG4-S-S-PEG4-acid
• Acid-PEG6-SS-PEG6-acid
• Amino-SS-PEG12-acid
• Aminoethyl-SS-ethylalcohol
• Aminoethyl-SS-ethylamine
• Aminoethyl-SS-propionic acid
• Azido-PEG3-SS-PEG3-azide
• Azido-SS-PEG2-acid
• Azidoethyl-PEG2-t-Butyl ester
• Azidoethyl-SS-ethylalcohol
• Azidoethyl-SS-ethylamine
• Azidoethyl-SS-ethylazide
• Azidoethyl-SS-propionic acid
• Azidoethyl-SS-propionic NHS ester
• Biotin-bisamido-SS-NHS
• Bis-Tos-(2-hydroxyethyl disulfide)
• Boc-aminooxy-ethyl-SS-propanol
• Boc-NH-ethyl-SS-propionic acid
• Fmoc-NH-ethyl-SS-propionic acid
• Fmoc-NH-ethyl-SS-propionic NHS ester
• Hydroxy-PEG3-SS-PEG3-alcohol
• m-PEG6-SS-PEG6-methyl
• Mal-NH-ethyl-SS-propionic acid
• NThiol-SS-biotin
• Propargyl-PEG1-SS-alcohol
• Propargyl-PEG1-SS-PEG1-acid
• Propargyl-PEG1-SS-PEG1-PFP ester
• Propargyl-PEG1-SS-PEG1-propargyl
• Propargyl-PEG1-SS-PEG1-t-butyl ester
• Sulfo-NThiol-SS-biotin
• t-Boc-Cystamine
• THP-SS-alcohol
• THP-SS-PEG1-t-butyl ester
• THP-SS-PEG1-Tos

Key benefits:

• Intracellular drug release rate is higher
• High bioavailability and biocompatibility
• Disulfide bonds are not toxic in vivo
• The fracture of disulfide bond can reduce the toxicity of polymer drugs
• Interact with or to manipulate the biological target
• Suitable for in vitro and in vivo experiments
• Ready-to-use

Application candidates:

• As an on-off switch for the release of antitumor drugs
• As a crosslinking agent to improve the stability of nanoparticles
• As a linking agent to construct nano-drug carrier
• As transfection vectors to deliver DNA and siRNA
• Be reactive groups for protein crosslinking, ligation or for click chemistry
• Fluorescent probes for diagnostic tools, proteomic analysis or cell imaging