Degrader Building Blocks

Targeted protein degradation can be achieved using heterobifunctional small molecule degraders, which are modular in design, comprising binding moieties for an E3 ubiquitin ligase and a target protein joined by a linker. Below you will find a toolbox of degrader building blocks to support targeted protein degradation research and development.

Products
Background
Literature

Functionalized E3 Ligase Ligands

Cat No Product Name / Activity
6466 TC E3 5031
Carboxylic acid-functionalized Thalidomide; cereblon ligand for PROTACs
6628 TC E3 5032
Precursor to Pomalidomide-based PROTACs
6685 Thalidomide, propargyl
Alkyne-functionalized Thalidomide; 'click' cereblon ligand for PROTACs
6462 VH 032, amine hydrochloride
Functionalized VHL ligand for PROTACs
6683 VH 032, propargyl
Alkyne-functionalized VH 032; 'click' VHL ligand for PROTACs

Cereblon Targeting Ligands Plus Linkers

Cat No Product Name / Activity
6300 Azido-Thalidomide
Thalidomide-alkylC4-Azide
6637 Pomalidomide - linker 1
Pomalidomide-PEG2-ethylamine
6681 Pomalidomide - linker 2
Pomalidomide-PEG3-carboxylic acid
6682 Pomalidomide - linker 3
Pomalidomide-alkylC5-carboxylic acid
6467 Thalidomide - linker 1
Thalidomide-PEG3-ethylamine
6468 Thalidomide - linker 2
Thalidomide-PEG4-ethylamine
6469 Thalidomide - linker 3
Thalidomide-alkylC4-amine
6627 Thalidomide - linker 4
Thalidomide-alkylC6-amine
6686 Thalidomide - linker 5
Thalidomide-PEG2-alkyne

VHL Targeting Ligands Plus Linkers

Cat No Product Name / Activity
6463 VH 032 - linker 1
VH 032-PEG3-amine
6464 VH 032 - linker 2
VH 032-PEG4-amine
6465 VH 032 - linker 3
VH 032-alkylC4-amine
6680 VH 032 - linker 5
VH 032-alkylC4-terminal carboxylic acid
6684 VH 032 - linker 6
VH 032-PEG2-alkyne

Functionalized Warhead Ligands

Cat No Product Name / Activity
6588 (+)-JQ1 carboxylic acid
Carboxylic acid-functionalized BET bromodomain inhibitor; target ligand for PROTACs
6589 (+)-JQ1 PA
Functionalized BET bromodomain inhibitor; 'click' target ligand for PROTACs

Related Categories

    Heterobifunctional small molecule degraders (e.g. PROTACs™) induce targeted protein degradation and are modular in design, consisting of three covalently linked components:

    • E3 ubiquitin ligase ligand
    • Linker
    • Ligand for a target protein of interest

    They have successfully been designed and utilized to induce targeted degradation of a variety of different proteins, including bromodomain-containing proteins, ligases, kinases, and RTKs. Application of this approach to achieve knockdown of further targets is currently an area of active research.

    Tocris provides building blocks to support Degrader research and development. Our range of Degrader components have functional handles for easy conjugation to ligands/linkers of interest. Included in this range are 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.

    PROTAC is a registered trademark of Arvinas, Inc.

    Require a different derivative? Get in touch.

    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.


    New Product Guide

    New Product Guide (Fall/Winter 2018/2019)

    Our new product guide highlights over 190 new products added to the Tocris Bioscience range during the second half of 2018.

    • 7-TM Receptors
    • Enzymes
    • Enzyme-Linked Receptors
    • Ion Channels
    • Nuclear Receptors
    • Transporters
    • Chemogenetics
    • Epigenetics
    • Fluorescent Imaging
    • PROTACs
    • Signal Transduction
    • Stem Cells