Degrader Building Blocks

Tocris provides Building Blocks to support Degrader research and development. Degraders (e.g. PROTAC® molecules, 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. You can also select your own panel of E3 ligase ligands + linkers for your Degrader development program using our new PROTAC Panel Builder tool.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Targets
Literature (4)

Related Categories

    VHL Targeting Ligands Plus Linkers

    Cat. No. Product Name Structure E3 Ligase Exit Vector Linker
    Type
    Number
    of Units
    Conjugation
    Functionality
    7104 VH 032 amide-PEG1-acid Cat.No. 7104 - VH 032 amide-PEG1-acid Tools for Targeted Protein Degradation PEG 1 Acid
    6879 VH 032 amide-PEG1-amine Cat.No. 6879 - VH 032 amide-PEG1-amine Tools for Targeted Protein Degradation PEG 1 Amine
    6907 VH 032 amide-PEG2-amine Cat.No. 6907 - VH 032 amide-PEG2-amine Tools for Targeted Protein Degradation PEG 2 Amine
    6684 VH 032 amide-PEG2-alkyne Cat.No. 6684 - VH 032 amide-PEG2-alkyne Tools for Targeted Protein Degradation PEG 2 Alkyne
    6679 VH 032 amide-PEG3-acid Cat.No. 6679 - VH 032 amide-PEG3-acid Tools for Targeted Protein Degradation PEG 3 Carboxylic Acid
    6463 VH 032 amide-PEG3-amine Cat.No. 6463 - VH 032 amide-PEG3-amine Tools for Targeted Protein Degradation PEG 3 Amine
    6464 VH 032 amide-PEG4-amine Cat.No. 6464 - VH 032 amide-PEG4-amine Tools for Targeted Protein Degradation PEG 4 Amine
    7106 VH 032 amide-alkylC2-acid Cat.No. 7106 - VH 032 amide-alkylC2-acid Tools for Targeted Protein Degradation Alkyl 2 Carboxylic Acid
    6852 VH 032 amide-alkylC2-amine Cat.No. 6852 - VH 032 amide-alkylC2-amine Tools for Targeted Protein Degradation Alkyl 2 Amine
    6680 VH 032 amide-alkylC4-acid Cat.No. 6680 - VH 032 amide-alkylC4-acid Tools for Targeted Protein Degradation Alkyl 4 Carboxylic Acid
    6465 VH 032 amide-alkylC4-amine Cat.No. 6465 - VH 032 amide-alkylC4-amine Tools for Targeted Protein Degradation Alkyl 4 Amine
    6985 VH 032 amide-alkylC5-amine Cat.No. 6985 - VH 032 amide-alkylC5-amine Tools for Targeted Protein Degradation Alkyl 5 Amine
    7107 VH 032 amide-alkylC6-acid Cat.No. 7107 - VH 032 amide-alkylC6-acid Tools for Targeted Protein Degradation Alkyl 6 Carboxylic Acid
    6853 VH 032 amide-alkylC6-amine Cat.No. 6853 - VH 032 amide-alkylC6-amine Tools for Targeted Protein Degradation Alkyl 6 Amine
    7074 VH 032 amide-alkylC7-amine Cat.No. 7074 - VH 032 amide-alkylC7-amine Tools for Targeted Protein Degradation Alkyl 7 Amine
    7108 VH 032 amide-alkylC8-acid Cat.No. 7108 - VH 032 amide-alkylC8-acid Tools for Targeted Protein Degradation Alkyl 8 Carboxylic Acid
    6890 VH 032 amide-alkylC8-amine Cat.No. 6890 - VH 032 amide-alkylC8-amine Tools for Targeted Protein Degradation Alkyl 8 Amine
    6880 VH 032 amide-alkylC10-amine Cat.No. 6880 - VH 032 amide-alkylC10-amine Tools for Targeted Protein Degradation Alkyl 10 Amine
    6909 VH 032 phenol-alkylC4-amine Cat.No. 6909 - VH 032 phenol-alkylC4-amine Tools for Targeted Protein Degradation Alkyl 4 Amine
    6910 VH 032 phenol-alkylC6-amine Cat.No. 6910 - VH 032 phenol-alkylC6-amine Tools for Targeted Protein Degradation Alkyl 6 Amine
    7293 VH 101 phenol-alkylC4-amine Cat.No. 7293 - vh-101-phenol-alkylc4-amine Tools for Targeted Protein Degradation Alkyl 4 Amine

    Cereblon Targeting Ligands Plus Linkers

    Cat. No. Product Name Structure E3 Ligase Exit Vector Linker
    Type
    Number
    of Units
    Conjugation
    Functionality
    7075 Lenalidomide 4'-PEG1-amine Cat.No. 7075 - Lenlidomide 4'-PEG1-amine - PEG 2 Amine
    7093 Lenalidomide 4'-PEG2-amine Cat.No. 7093 - Lenlidomide 4'-PEG2-amine - PEG 2 Amine
    7076 Lenalidomide 4'-PEG3-amine Cat.No. 7076 - Lenlidomide 4'-PEG3-amine - PEG 3 Amine
    7094 Pomalidomide 4'-PEG1-acid Cat.No. 7094 - Pomalidomide 4'-PEG1-acid - PEG 1 Acid
    7212 Pomalidomide 4'-PEG2-acid Cat.No. 7212 - Pomalidomide 4'-PEG2-acid - PEG 2 Acid
    7095 Pomalidomide 4'-PEG5-acid Cat.No. 7095 - Pomalidomide 4'-PEG5-acid - PEG 5 Acid
    6637 Pomalidomide 4'-PEG2-amine Cat.No. 6637 - Pomalidomide 4'-PEG2-amine - PEG 2 Amine
    6681 Pomalidomide 4'-PEG3-acid Cat.No. 6681 - Pomalidomide 4'-PEG3-acid - PEG 3 Carboxylic Acid
    7096 Pomalidomide 4'-alkylC3-acid Cat.No. 7096 - Pomalidomide 4'-alkylC3-acid - Alkyl 3 Carboxylic Acid
    7209 Pomalidomide 4'-alkylC4-acid Cat.No. 7209 - Pomalidomide 4'-alkylC4-acid - Alkyl 4 Carboxylic Acid
    6682 Pomalidomide 4'-alkylC5-acid Cat.No. 6682 - Pomalidomide 4'-alkylC5-acid - Alkyl 5 Carboxylic Acid
    7210 Pomalidomide 4'-alkylC6-acid Cat.No. 7210 - Pomalidomide 4'-alkylC6-acid - Alkyl 6 Carboxylic Acid
    7097 Pomalidomide 4'-alkylC7-acid Cat.No. 7097 - Pomalidomide 4'-alkylC7-acid - Alkyl 7 Carboxylic Acid
    7211 Pomalidomide 4'-alkylC8-acid Cat.No. 7211 - Pomalidomide 4'-alkylC8-acid - Alkyl 8 Carboxylic Acid
    6851 Pomalidomide 4'-alkylC2-amine Cat.No. 6851 - Pomalidomide 4'-alkylC2-amine - Alkyl 2 Amine
    7205 Pomalidomide 4'-alkylC3-amine Cat.No. 7205 - Pomalidomide 4'-alkylC3-amine - Alkyl 3 Amine
    6716 Pomalidomide 4'-alkylC5-amine Cat.No. 6716 - Pomalidomide 4'-alkylC5-amine - Alkyl 5 Amine
    7208 Pomalidomide 4'-alkylC7-amine Cat.No. 7208 - Pomalidomide 4'-alkylC7-amine - Alkyl 7 Amine
    6944 Pomalidomide 4'-alkylC8-amine Cat.No. 6944 - Pomalidomide 4'-alkylC8-amine - Alkyl 8 Amine
    7203 Pomalidomide 4'-PEG1-amine Cat.No. 7203 - Pomalidomide 4'-PEG1-amine - PEG 1 Ethylamine
    7204 Pomalidomide 4'-PEG3-amine Cat.No. 7204 - Pomalidomide 4'-PEG3-amine - PEG 3 Ethylamine
    6963 Pomalidomide 4'-PEG4-amine Cat.No. 6963 - Pomalidomide 4'-PEG4-amine - PEG 4 Ethylamine
    7329 Thalidomide 4'-ether-alkylC2-acid Cat.No. 7329 - Thalidomide 4'-ether-alkylC2-acid Tools for Targeted Protein Degradation Alkyl 2 Acid
    6850 Thalidomide 4'-ether-alkylC2-amine Cat.No. 6850 - Thalidomide 4'-ether-alkylC2-amine Tools for Targeted Protein Degradation Alkyl 2 Amine
    7330 Thalidomide 4'-ether-alkylC3-acid Cat.No. 7330 - Thalidomide 4'-ether-alkylC3-acid Tools for Targeted Protein Degradation Alkyl 3 Acid
    7331 Thalidomide 4'-ether-alkylC4-acid Cat.No. 7331 - Thalidomide 4'-ether-alkylC4-acid Tools for Targeted Protein Degradation Alkyl 4 Acid
    6917 Thalidomide 4'-ether-alkylC4-amine Cat.No. 6917 - Thalidomide 4'-ether-alkylC4-amine Tools for Targeted Protein Degradation Alkyl 4 Amine
    7332 Thalidomide 4'-ether-alkylC5-acid Cat.No. 7332 - Thalidomide 4'-ether-alkylC5-acid Tools for Targeted Protein Degradation Alkyl 5 Acid
    6627 Thalidomide 4'-ether-alkylC6-amine Cat.No. 6627 - Thalidomide 4'-ether-alkylC6-amine Tools for Targeted Protein Degradation Alkyl 6 Amine
    7333 Thalidomide 4'-ether-alkylC6-acid Cat.No. 7333 - Thalidomide 4'-ether-alkylC6-acid Tools for Targeted Protein Degradation Alkyl 6 Acid
    7334 Thalidomide 4'-ether-alkylC7-acid Cat.No. 7334 - Thalidomide 4'-ether-alkylC7-acid Tools for Targeted Protein Degradation Alkyl 7 Acid
    7335 Thalidomide 4'-ether-alkylC8-acid Cat.No. 7335 - Thalidomide 4'-ether-alkylC8-acid Tools for Targeted Protein Degradation Alkyl 8 Acid
    6686 Thalidomide 4'-ether-PEG2-alkyne Cat.No. 6686 - Thalidomide 4'-ether-PEG2-alkyne Tools for Targeted Protein Degradation PEG 2 Alkyne
    6950 Thalidomide 4'-ether-PEG3-amine Cat.No. 6850 - Thalidomide 4'-ether-PEG3-amine Tools for Targeted Protein Degradation PEG 3 Ethylamine
    6951 Thalidomide 4'-ether-PEG5-amine Cat.No. 6851 - Thalidomide 4'-ether-PEG5-amine Tools for Targeted Protein Degradation PEG 5 Ethylamine
    6949 Thalidomide 4'-oxyacetamide-alkylC2-amine Cat.No. 6849 - Thalidomide 4'-oxyacetamide-alkylC2-amine Tools for Targeted Protein Degradation Alkyl 2 Amine
    6469 Thalidomide 4'-oxyacetamide-alkylC4-amine Cat.No. 6469 - Thalidomide 4'-oxyacetamide-alkylC4-amine Tools for Targeted Protein Degradation Alkyl 4 Amine
    6968 Thalidomide 4'-oxyacetamide-alkylC6-amine Cat.No. 6968 - Thalidomide 4'-oxyacetamide-alkylC6-amine Tools for Targeted Protein Degradation Alkyl 6 Amine
    6946 Thalidomide 4'-oxyacetamide-alkylC8-amine Cat.No. 6946 - Thalidomide 4'-oxyacetamide-alkylC8-amine Tools for Targeted Protein Degradation Alkyl 2 Amine
    6300 Thalidomide 4'-oxyacetamide-alkylC4-azide Cat.No. 6300 - Thalidomide 4'-oxyacetamide-alkylC4-azide Tools for Targeted Protein Degradation Alkyl 4 Azide
    6966 Thalidomide 4'-oxyacetamide-PEG1-amine Cat.No. 6966 - Thalidomide 4'-oxyacetamide-PEG1-amine Tools for Targeted Protein Degradation PEG 1 Ethylamine
    6967 Thalidomide 4'-oxyacetamide-PEG2-amine Cat.No. 6967 - Thalidomide 4'-oxyacetamide-PEG2-amine Tools for Targeted Protein Degradation PEG 2 Ethylamine
    6467 Thalidomide 4'-oxyacetamide-PEG3-amine Cat.No. 6467 - Thalidomide 4'-oxyacetamide-PEG3-amine Tools for Targeted Protein Degradation PEG 3 Amine
    6468 Thalidomide 4'-oxyacetamide-PEG4-amine Cat.No. 6468 - Thalidomide 4'-oxyacetamide-PEG4-amine Tools for Targeted Protein Degradation PEG 4 Amine
    6913 Thalidomide 4'-oxyacetamide-alkylC1-PEG3-alkylC3-amine Cat.No. 6913 - Thalidomide 4 Tools for Targeted Protein Degradation Alkyl-PEG-Alkyl 1-3-3 Amine

    IAP Targeting Ligands Plus Linkers

    Cat. No. Product Name Structure E3 Ligase Exit Vector Linker
    Type
    Number
    of Units
    Conjugation
    Functionality
    6474 A 410099.1 amide-alkylC4-amine Cat.No. 6474 - A 410099.1 amide-alkylC4-amine Tools for Targeted Protein Degradation Amide-Alkyl 4 Amine
    6473 A 410099.1 amide-PEG2-amine Cat.No. 6473 - A 410099.1 amide-PEG2-amine Tools for Targeted Protein Degradation Amide-PEG 2 Amine
    6472 A 410099.1 amide-PEG3-amine Cat.No. 6472 - A 410099.1 amide-PEG3-amine Tools for Targeted Protein Degradation Amide-PEG 3 Amine
    7220 A 410099.1 amide-PEG4-amine Cat.No. 7220 - A 410099.1 amide-PEG4-amine Tools for Targeted Protein Degradation Amide-PEG 4 Amine
    7221 A 410099.1 amide-PEG5-amine Cat.No. 7221 - A 410099.1 amide-PEG5-amine Tools for Targeted Protein Degradation Amide-PEG 5 Amine

    Functionalized E3 Ligase Ligands

    Cat. No. Product Name Structure E3 Ligase Ligand Target E3 Reactive Handle Reaction Chemistry
    6471 A 410099.1, amine Cat.No. 6471 - A 410099.1, amine A 410099.1 IAP Primary Amine Amide coupling
    7178 LCL 161, phenol Cat.No. 7178 - LCL 161, phenol LCL 161 IAP Alcohol Mitsunobu reaction
    6466 TC E3 5031 Cat.No. 6466 - TC E3 5031 Thalidomide Cereblon Carboxylic acid Amide coupling
    6628 TC E3 5032 Cat.No. 6628 - TC E3 5032 Pomalidomide Cereblon Fluorine Nucleophilic aromatic substitution
    6685 Thalidomide, propargyl Cat. No. 6685 - Thalidomide, propargyl Thalidomide Cereblon Alkyne Click chemistry
    6462 VH 032, amine Cat. No. 6462 - VH 032, amine VH 032 VHL Primary amine Amide coupling
    6969 cis VH 032, amine dihydrochloride Cat. No. 6969 - cis VH 032, amine dihydrochloride VH 032 VHL Primary amine Amide coupling
    6911 VH 032, phenol Cat. No. 6911 - VH 032, phenol VH 032 VHL Alcohol Mitsunobu reaction
    6683 VH 032, propargyl Cat. No. 6683 - VH 032, propargyl VH 032 VHL Alkyne Click chemistry
    6952 VH 101, phenol Cat. No. 6952 - VH 101, phenol VH 101 VHL Alcohol Mitsunobu reaction

    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 JQ1 BET Bromodomains Carboxylic acid Amide coupling
    6589 (+)-JQ1 PA Cat. No. 6589 - (+)-JQ1 PA JQ1 BET Bromodomains Alkyne Click chemistry

    Require a different derivative? Get in touch.

    PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

    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
    • Degrader Building Blocks
    • Custom Degrader Services
    • UPS Proteins and Assays
    • Assays for Protein Degradation
    Developing Degraders

    Developing Degraders Poster

    This poster describes the generation of a database of Degraders (PROTACs®) from the literature. The Degraders were profiled according to the constituent ligands, linker type, linker length and physicochemical properties and this information was used to establish a set of guidelines for the design and synthesis of cell-permeable Degrader molecules. Presented at the 20th SCI/RSC Medicinal Chemistry Symposium 2019, Cambridge, UK.

    PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

    Enabling Research By Provision of Chemical Tools

    Enabling Research By Provision of Chemical Tools Poster

    The Tocris chemistry team has considerable chemistry knowledge and skill which it has recently been applying to the generation of new chemical probes from known tools and compounds to help answer biological questions. This poster presents some of the work carried out by Tocris scientists and focuses on two areas: the generation of libraries of chemical building blocks to support Degrader (PROTAC) research and the development of a fluorescent probe to study integrin biology. Presented at Chemical Tools for Complex Biological Systems II, 2019, Janelia Research Campus, USA.
    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. Presented at EFMC 2018, Ljubljana, Slovenia