Mal-amido-PEG2-TFP ester is a heterobifunctional polyethylene glycol linker designed for PROTAC and related targeted degradation workflows, combining a maleimide-reactive handle with an amide-linked short PEG spacer and a terminal N-hydroxysuccinimide (NHS, TFP) ester for acylation of primary amines. The PEG2 segment provides aqueous solubility and a modest, flexible distance between the two reactive termini, which can reduce steric interference during conjugation. In PROTAC construction, the maleimide group enables chemoselective coupling to thiol-containing ligands (e.g., cysteine residues on proteins or thiol-functionalized targeting moieties) via Michael-type addition, while the TFP ester efficiently forms stable amide bonds with lysine or N-terminal amines on the complementary component. This dual reactivity supports modular assembly of degraders, facilitating rapid generation of conjugates with controlled geometry and improved handling for downstream binding and degradation assays.
Structure of 1431291-44-9
* For research and manufacturing use only. Not for human or clinical use.
| Size | Price | Stock | Quantity |
|---|---|---|---|
| -- | $-- | In stock |
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| ConcentrationVolumeMass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.0992 mL | 10.4958 mL | 20.9916 mL |
| 5 mM | 0.4198 mL | 2.0992 mL | 4.1983 mL |
| 10 mM | 0.2099 mL | 1.0496 mL | 2.0992 mL |
This Mal-amido-PEG2-TFP ester is a bifunctional PROTAC linker designed to connect a maleimide-bearing handle with an activated carboxylate for efficient conjugation. Its PEG spacer supports favorable solubility and conformational flexibility, while the TFP ester enables rapid acylation of nucleophilic groups on targeting ligands. The combination of orthogonal reactivity makes it suitable for assembling targeted protein degradation constructs; the detailed structural and reactivity features are described below.
Structure: The linker contains a maleimide moiety for chemoselective Michael-type addition, an amide linkage, and a short polyethylene glycol spacer that increases hydrophilicity. An activated TFP ester provides an electrophilic carbonyl for acyl transfer, with stable covalent bonds formed upon conjugation.
Reactivity: Use the TFP ester for coupling to primary amines or other suitable nucleophiles under mild, anhydrous-to-semi-aqueous conditions, typically with base to promote nucleophile activation. The maleimide reacts via Michael addition with thiols (or thiol-containing ligands) to form a stable thioether. Perform sequential or orthogonal conjugations by controlling order, pH, and solvent compatibility; common coupling solvents include DMF or DMSO, with careful exclusion of competing thiols during TFP activation.
* 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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