Folate-PEG1-mal

 Cat No.: BP-501918 4.5  

Folate-PEG1-mal is a heterobifunctional PROTAC linker built on a short polyethylene glycol spacer bearing a terminal maleimide (mal) for selective conjugation and a folate recognition motif for targeting folate-receptor–expressing systems. Structurally, it combines a folate headgroup with a PEG1 chain that provides modest hydrophilicity and spatial separation, while the maleimide electrophile enables chemoselective coupling to thiol-containing partners (for example, cysteine residues or thiol-functionalized ligands) via stable thioether bond formation. In PROTAC or targeted degradation workflows, this linker can be used to tether a folate-based targeting ligand to a second module, such as an E3 ligase binder or a reactive handle-bearing degrader scaffold, thereby promoting proximity-driven recruitment and facilitating ternary-complex formation. Its value lies in enabling modular assembly of folate-receptor–directed degraders with controlled conjugation chemistry and reduced steric interference, supporting systematic structure–activity optimization in targeted protein degradation research.

Folate-PEG1-mal

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PROTAC Linker
Molecular Formula
C₂₇H₂₈N₈O₉
Molecular Weight
608.56

* For research and manufacturing use only. Not for human or clinical use.

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Please store the product under the recommended conditions in the Certificate of Analysis.
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IUPACName
(2S)-2-[4-[(2-amino-4-oxo-3H-pteridin-6-yl)methylamino]benzoyl]oxy-5-[2-[2-(2,5-dioxopyrrol-1-yl)ethoxy]ethylamino]-5-oxopentanoic acid
InChI Key
BJHACKFMUSRLKU-SFHVURJKSA-N
InChI
InChI=1S/C27H28N8O9/c28-27-33-23-22(24(39)34-27)32-17(14-31-23)13-30-16-3-1-15(2-4-16)26(42)44-18(25(40)41)5-6-19(36)29-9-11-43-12-10-35-20(37)7-8-21(35)38/h1-4,7-8,14,18,30H,5-6,9-13H2,(H,29,36)(H,40,41)(H3,28,31,33,34,39)/t18-/m0/s1
SMILES
C1=CC(=CC=C1C(=O)OC(CCC(=O)NCCOCCN2C(=O)C=CC2=O)C(=O)O)NCC3=CN=C4C(=N3)C(=O)NC(=N4)N

This Folate-PEG1-mal linker is designed to connect a folate-derived targeting motif to a PROTAC-relevant functional handle, enabling efficient assembly of targeted protein degraders through modular conjugation. Its PEG-based spacer supports favorable solubility and conformational flexibility, while the malemide functionality provides a robust platform for forming stable linkages under standard bioconjugation practices. The sections below describe the linker’s structure and the practical reactivity considerations for PROTAC construction.

Structure: The linker contains a short polyethylene glycol spacer that confers hydrophilicity and spacing between conjugated fragments. It incorporates a malemide (maleimide) electrophilic group capable of selective nucleophile addition, alongside a folate-derived targeting element for receptor-mediated recognition. The scaffold features stable covalent linkages suitable for PROTAC assembly.

Reactivity: Malemide groups typically undergo Michael-type addition with thiol-containing nucleophiles, enabling conjugation to cysteine-bearing ligands or thiolated intermediates. For PROTAC synthesis, reactions are commonly performed under mildly basic, aqueous or mixed-solvent conditions to maintain thiol nucleophile availability while minimizing side reactions. Solvent systems that preserve solubility of both partners are preferred, and catalysts are generally not required; careful control of pH and thiol stoichiometry supports selective coupling.

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L

* 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

* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O √ c22h30n40 ╳
g/mol
g

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