Cleavable Linkers

CD Bioparticles has an advanced and customizable drug delivery platform to help you solve all the problems of drug delivery in one stop. We provide high-quality cleavable linkers for carrier and drug conjugation, which can help you solve:

Figure 1. Cleavable linkers. (Tsuchikama K, et al.; 2018)Figure 1. Cleavable linkers. (Tsuchikama K, et al.; 2018)

The challenges you might meet:

  • The drug delivery system cannot control release, has strong off-target effects, and has poor therapeutic effects.
  • Contains drugs that are susceptible to degradation when exposed to blood or the surrounding environment
  • Drugs can cause side effects as they are distributed throughout the body
  • The contained drug has limited solubility, making formulating it for intravenous administration challenging
  • Drugs have shorter circulation time
  • In combination therapy, drugs need to be released sequentially or coordinatedly at the target site
  • Drugs developed are susceptible to drug resistance

Cleavable Linkers Key features:

  • PC Cleavable Linkers
    • PC Alkyne-PEG4-NHS carbonate ester
    • PC Azido-PEG11-NHS carbonate ester
    • PC Biotin-PEG3-alkyne
    • PC Biotin-PEG3-azide
    • PC Biotin-PEG3-NHS carbonate ester
    • PC DBCO-PEG3-biotin
    • PC Mal-NHS carbonate ester
    • PC Methyltetrazine-PEG4-NHS carbonate ester
    • PC SPDP-NHS carbonate ester
    • PC-Biotin-PEG4-NHS carbonate
    • PC-Biotin-PEG4-PEG3-azide
    • PC-Biotin-PEG4-PEG4-alkyne
  • Dde Cleavable Linkers
    • Dde Biotin-PEG4-alkyne
    • Dde Biotin-PEG4-azide
    • Dde Biotin-PEG4-DBCO
    • Dde Biotin-PEG4-Picolyl azide
  • β-Glucuronide Linkers
    • (2S,3S,4S,5R,6S)-methyl-6-(2-(3-((Fmoc-amino) propanamido)-4-PNP-3,4,5-triacetoxy-tetrahydro-2H-pyran-2-carboxylate
    • 4-Formyl-2-nitrophenyl-β-D-Glucopyranosiduronic Acid Methyl Ester 2,3,4-Triacetate
    • β-D-Glucopyranosiduronic acid, 2-amino-4-(hydroxymethyl)phenyl, methyl ester, 2,3,4-triacetate
    • β-D-tetraacetylgalactopyranoside-PEG2-azide
    • β-D-triacetylglucopyranosiduronyl methyl ester-phenol-β-Alanine
    • β-tetraacetylglucopyranoside-glycerol
    • β-tetraacetylglucopyranoside-glycol
  • -S-S- Cleavable Linkers
    • 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
  • Cleavable Peptide Linkers
  • Diazo Biotin Cleavable Linkers
    • Diazo Biotin-PEG3-alkyne
    • Diazo Biotin-PEG3-azide
    • Diazo Biotin-PEG3-DBCO

Cleavable Linkers Key benefits:

  • Low immunogenicity
  • Intracellular drug release rate is higher
  • Interact with or to manipulate the biological target
  • Rupture resistance and specific cracking conditions
  • The structure does not affect the activity of other proteases
  • High tumor affinity and specificity
  • Increase the hydrophilicity of the loaded drugs
  • High bioavailability and biocompatibility
  • Mild cracking conditions
  • Suitable for in vitro and in vivo experiments
  • Ready-to-use

Cleavable Linkers 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
  • Construction and application of peptide/protein-conjugated drugs
  • Tags for MS analysis or purification
  • Study on metabolism of glucuronidation and drug metabolism in vivo
  • Investigate the role of linker chemistry in enhancing drug efficacy, increasing cycle time and reducing toxicity
  • Fluorescent probes for diagnostic tools, proteomic analysis or cell imaging
  • Protein–protein interactions
  • Activity-based protein profiling
  • Elucidation of drug targets and their binding sites
  • Study on covalent metabolite interactions


  1. Tsuchikama K, An Z. Antibody-drug conjugates: recent advances in conjugation and linker chemistries. Protein Cell. 2018, 9(1):33-46.
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