2-(Biotin-amido)-1,3-bis-(C1-PEG1-acid)
2-(Biotin-amido)-1,3-bis-(C1-PEG1-acid) is a bifunctional PROTAC linker building block that combines a biotin–amide handle with two short, hydrophilic C1 PEG1 carboxylic acid termini arranged on a 1,3-bis-substituted scaffold. The PEG-based segments provide aqueous solubility and conformational flexibility, while the biotin–amide motif enables strong, selective noncovalent capture by streptavidin or related biotin-binding proteins, which is useful for affinity-based visualization, enrichment, and pull-down workflows during linker optimization. In targeted protein degradation designs, this type of linker can serve as a spacer that positions two reactive conjugation points for attachment to ligands (e.g., an E3 ligase recruiter and a target-binding moiety), thereby promoting productive ternary complex formation and improving the probability of ubiquitination. Its dual functional groups and solubility-enhancing PEG units make it valuable for systematic SAR studies where linker length, polarity, and geometry are tuned to balance degradation potency and construct stability.
Structure of 2086689-02-1
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2-(Biotin-amido)-1,3-bis-(C1-PEG1-acid), is designed to provide a biotin-containing anchoring handle alongside hydrophilic PEG-based spacers and carboxylic acid functionality. Its balanced polarity and functional-group density support efficient conjugation to targeting ligands and facilitate subsequent assembly of degradation constructs. The linker’s features are particularly useful in PROTAC workflows where controlled linker geometry and reliable amide/ester coupling chemistry are required; detailed structural and reactivity considerations are provided below.
Structure: The molecule contains an amide linkage connecting a biotin-derived moiety, flanked by a substituted 1,3-bis framework bearing short PEG units terminated with carboxylic acid groups. Multiple heteroatoms (including oxygen and nitrogen) provide strong hydrogen-bonding capacity and overall hydrophilicity.
Reactivity: The carboxylic acids enable standard PROTAC-building couplings to amines or alcohols via activated ester or carbodiimide-mediated pathways. Typical strategies involve pre-activation of the acid (for example, using carbodiimides with coupling additives) followed by nucleophilic substitution to form amide or related linkages. Mild bases and polar aprotic solvents are commonly used to preserve PEG integrity and minimize side reactions during assembly.
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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