Degrader Building Blocks

Tocris provides Building Blocks to support Degrader research and development. Degraders (e.g. PROTACsTM, SNIPERs etc) are heterobifunctional small molecules that are modular in design, comprising binding moieties for an E3 ubiquitin ligase and a target protein joined by a linker. Our Degrader components have functional handles for easy conjugation to ligands/linkers of interest. The range includes the most effective and commonly used E3 ubiquitin ligase ligands, functionalized at positions known not to interfere with binding affinity. E3 ligase ligands conjugated to common linker groups are also supplied. Below you will find a toolbox of Degrader Building Blocks to support targeted protein degradation research and development.

PROTAC is a registered trademark of Arvinas, Inc.

Targets
Literature

Related Categories

    VHL Targeting Ligands Plus Linkers

    Cat. No. Product Name Structure E3 Ligase Exit Vector Linker
    Type
    Number
    of Units
    Conjugation
    Functionality
    6463 VH 032 - linker 1 Cat.No. 6463 - VH 032 - linker 1 | C30H45N5O7S.HCl | CAS No. 2097971-11-2 Tools for Targeted Protein Degradation PEG 3 Amine
    6464 VH 032 - linker 2 Cat.No. 6464 - VH 032 - linker 2 | C32H49N5O8S.HCl | CAS No. 2064292-52-8 Tools for Targeted Protein Degradation PEG 4 Amine
    6465 VH 032 - linker 3 Cat.No. 6465 - VH 032 - linker 3 | C27H39N5O4S.HCl Tools for Targeted Protein Degradation Alkyl 4 Amine
    6680 VH 032 - linker 5 Cat.No. 6680 - VH 032 - linker 5 | C28H38N4O6S | CAS No. 2172819-74-6 Tools for Targeted Protein Degradation Alkyl 4 Carboxylic Acid
    6684 VH 032 - linker 6 Cat.No. 6684 - VH 032 - linker 6 | C31H42N4O7S | CAS No. 2098799-80-3 Tools for Targeted Protein Degradation PEG 2 Alkyne
    6853 VH 032 - linker 8 Cat.No. 6853 - VH 032 - linker 8 | C29H43N5O4S Tools for Targeted Protein Degradation Alkyl 6 Amine
    6879 VH 032 - linker 9 Cat.No. 6879 - VH 032 - linker 9 | C26H37N5O5S Tools for Targeted Protein Degradation PEG 1 Amine
    6880 VH 032 - linker 10 Cat.No. 6880 - VH 032 - linker 10 | C33H51N5O4S Tools for Targeted Protein Degradation Alkyl 10 Amine
    6890 VH 032 - linker 11 Cat.No. 6890 - VH 032 - linker 11 | C31H47N5O4S Tools for Targeted Protein Degradation Alkyl 8 Amine

    Cereblon Targeting Ligands Plus Linkers

    Cat. No. Product Name Structure E3 Ligase Exit Vector Linker
    Type
    Number
    of Units
    Conjugation
    Functionality
    6637 Pomalidomide - linker 1 Cat.No. 6637 - Pomalidomide - linker 1 | C19H24N4O6.HCl - PEG 2 Amine
    6681 Pomalidomide - linker 2 Cat.No. 6681 - Pomalidomide - linker 2 | C22H27N3O9 - PEG 3 Carboxylic Acid
    6682 Pomalidomide - linker 3 Cat.No. 6682 - Pomalidomide - linker 3 | C19H21N3O6 - Alkyl 5 Carboxylic Acid
    6851 Pomalidomide - linker 7 Cat.No. 6851 - Pomalidomide - linker 7 | C15H16N4O4.HCl - Alkyl 2 Amine
    6467 Thalidomide - linker 1 Cat.No. 6467 - Thalidomide - linker 1 | C23H30N4O9.HCl Tools for Targeted Protein Degradation PEG 3 Amine
    6468 Thalidomide - linker 2 Cat.No. 6468 - Thalidomide - linker 2 | C25H34N4O10.HCl Tools for Targeted Protein Degradation PEG 4 Amine
    6469 Thalidomide - linker 3 Cat.No. 6469 - Thalidomide - linker 3 | 	C19H22N4O6.HCl Tools for Targeted Protein Degradation Alkyl 4 Amine
    6627 Thalidomide - linker 4 Cat.No. 6627 - Thalidomide - linker 4 | 		C19H23N3O5.HCl Tools for Targeted Protein Degradation Alkyl 6 Amine
    6686 Thalidomide - linker 5 Cat.No. 6686 - Thalidomide - linker 5 | 		C20H20N2O7 Tools for Targeted Protein Degradation PEG 2 Alkyne
    6850 Thalidomide - linker 6 Cat.No. 6850 - Thalidomide - linker 6 | 		C15H15N3O5.HCl Tools for Targeted Protein Degradation Alkyl 2 Amine
    6300 Azido-Thalidomide Cat.No. 6300 - Azido-Thalidomide | 	C19H20N6O6 Tools for Targeted Protein Degradation Alkyl 4 Azide

    Functionalized E3 Ligase Ligands

    Cat. No. Product Name Structure E3 Ligase Ligand Target E3 Reactive Handle Reaction Chemistry
    6466 TC E3 5031 Cat.No. 6466 - TC E3 5031 | C15H12N2O7 | CAS No. 1061605-21-7 Thalidomide Cereblon Carboxylic acid Amide coupling
    6628 TC E3 5032 Cat.No. 6628 - TC E3 5032 | C13H9FN2O4 | CAS No. 835616-60-9 Pomalidomide Cereblon Fluorine Nucleophilic aromatic substitution
    6685 Thalidomide, propargyl Cat. No. 6685 - Thalidomide, propargyl | C16H12N2O5 | CAS No. 2098487-39-7 Thalidomide Cereblon Alkyne Click chemistry
    6462 VH 032, amine hydrochloride Cat. No. 6462 - VH 032, amine hydrochloride | C22H30N4O3S.HCl | CAS No. 1448189-80-7 VH 032 VHL Primary amine Amide coupling
    6683 VH 032, propargyl Cat. No. 6683 - VH 032, propargyl | C27H34N4O5S.HCl | CAS No. 2098799-78-9-7 VH 032 VHL Alkyne Click chemistry

    Functionalized Warhead Ligands

    Cat. No. Product Name Structure Ligand Target Protein Reactive Handle Reaction Chemistry
    6588 (+)-JQ1 carboxylic acid Cat. No. 6588 - (+)-JQ1 carboxylic acid | C19H17ClN4O2S | CAS No. 202592-23-2 JQ1 BET Bromodomains Carboxylic acid Amide coupling
    6589 (+)-JQ1 PA Cat. No. 6589 - (+)-JQ1 PA | C22H20ClN5OS | CAS No. 2115701-93-2 JQ1 BET Bromodomains Alkyne Click chemistry

    Require a different derivative? Get in touch.

    PROTAC is a registered trademark of Arvinas, Inc.

    Literature for Degrader Building Blocks

    Tocris offers the following scientific literature for Degrader Building Blocks to showcase our products. We invite you to request* or download your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


    Targeted Protein Degradation

    Targeted Protein Degradation Research Product Guide

    This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

    • Active Degraders (e.g. PROTACs)
    • Degrader Building Blocks
    • Custom Degrader Services
    • UPS Proteins and Assays
    • Assays for Protein Degradation
    Targeted Protein Degradation

    Targeted Protein Degradation Poster

    Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed.