PROTAC

PROTACs (Proteolysis Targeting Chimeras) are heterobifunctional molecules designed to induce selective degradation of disease-related proteins. A typical PROTAC consists of a ligand for the target protein, a ligand for an E3 ubiquitin ligase, and a linker connecting the two. By bringing the target protein into proximity with the E3 ligase, PROTAC molecules promote ubiquitination and subsequent degradation of the protein by the proteasome.

Unlike traditional inhibitors, PROTACs eliminate target proteins rather than simply blocking their activity. This catalytic degradation mechanism enables sustained biological effects and allows access to targets previously considered difficult to drug. The rapid expansion of PROTAC pipelines across oncology, immunology, and other therapeutic areas highlights its potential as a next-generation modality in drug discovery.

製品一覧

カタログ番号	名称	CAS番号	分子量
CH56001	Boc-NH-PEG2-C2-NH2	153086-78-3	248.32
CH56002	Bis(2-bromoethyl) ether	5414-19-7	231.91
CH56003	Boc-NH-PEG2-CH2COOH	108466-89-3	263.29
CH56004	2-Chloroethanamine hydrochloride	870-24-6	115.99
CH56005	Hexane-1,6-diol	629-11-8	118.17
CH56006	Azido-PEG4-alcohol	86770-67-4	219.24
CH56007	Ethyl hydroxyacetate	623-50-7	104.1
CH56008	Methyl 3-hydroxypropanoate	6149-41-3	104.1
CH56009	2,2-Oxybis(ethylamine)	2752-17-2	104.15
CH56010	NH2-PEG4-CH2CH2COOH	663921-15-1	265.3

Technical Questions

Frequently Asked Questions

Common questions about custom synthesis, process development, analytical information, and project discussion for PROTAC.

What is the difference between PROTACs and molecular glues?

PROTACs are bifunctional with a defined linker between target ligand and E3 recruiter. Molecular glues are monomeric small molecules that induce protein-protein interactions between target and E3 ligase without an obvious linker. Lenalidomide and pomalidomide are classic molecular glues that recruit CRBN to neosubstrates.

When should I use CRBN vs VHL E3 recruiters?

CRBN-based recruiters (pomalidomide, lenalidomide) are smaller and synthetically accessible but carry risk of IMiD-related off-target degradation. VHL recruiters (VH032/AHPC) avoid IMiD mechanisms but are larger. Choice depends on target, tissue expression of the E3, and resistance considerations.

What linker length is optimal for PROTAC activity?

Optimal linker length and composition are highly target-specific. Typical PROTAC libraries screen PEG2 through PEG6 linkers plus alkyl variants. Rigid or branched linkers can improve ternary complex geometry for some targets.

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