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.
Cat. No. | Product Name | Structure | E3 Ligase Exit Vector | Linker
Type |
Number
of Units |
Conjugation
Functionality |
---|---|---|---|---|---|---|
7106 | VH 032 amide-alkylC2-acid |
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Alkyl | 2 | Carboxylic Acid |
6852 | VH 032 amide-alkylC2-amine |
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Alkyl | 2 | Amine |
7216 | VH 032 amide-alkylC3-acid |
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Alkyl | 3 | Acid |
7073 | VH 032 amide-alkylC3-amine |
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Alkyl | 3 | Amine |
6680 | VH 032 amide-alkylC4-acid |
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Alkyl | 4 | Carboxylic Acid |
6465 | VH 032 amide-alkylC4-amine |
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Alkyl | 4 | Amine |
7217 | VH 032 amide-alkylC5-acid |
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Alkyl | 5 | Acid |
6985 | VH 032 amide-alkylC5-amine |
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Alkyl | 5 | Amine |
7867 | VH 032 amide-alkylC5-azide |
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Alkyl | 5 | Azide |
7107 | VH 032 amide-alkylC6-acid |
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Alkyl | 6 | Carboxylic Acid |
6853 | VH 032 amide-alkylC6-amine |
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Alkyl | 6 | Amine |
7925 | VH 032 amide-alkylC7-acid |
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Alkyl | 7 | Carboxylic Acid |
7074 | VH 032 amide-alkylC7-amine |
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Alkyl | 7 | Amine |
7108 | VH 032 amide-alkylC8-acid |
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Alkyl | 8 | Carboxylic Acid |
6890 | VH 032 amide-alkylC8-amine |
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Alkyl | 8 | Amine |
7404 | VH 032 amide-alkylC9-acid |
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Alkyl | 9 | Carboxylic Acid |
7566 | VH 032 amide-alkylC9-amine |
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Alkyl | 9 | Amine |
6880 | VH 032 amide-alkylC10-amine |
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Alkyl | 10 | Amine |
7104 | VH 032 amide-PEG1-acid |
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PEG | 1 | Acid |
6879 | VH 032 amide-PEG1-amine |
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PEG | 1 | Amine |
6907 | VH 032 amide-PEG2-amine |
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PEG | 2 | Amine |
6684 | VH 032 amide-PEG2-alkyne |
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PEG | 2 | Alkyne |
6679 | VH 032 amide-PEG3-acid |
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PEG | 3 | Carboxylic Acid |
6463 | VH 032 amide-PEG3-amine |
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PEG | 3 | Amine |
7215 | VH 032 amide-PEG4-acid |
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PEG | 4 | Carboxylic Acid |
6464 | VH 032 amide-PEG4-amine |
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PEG | 4 | Amine |
7105 | VH 032 amide-PEG5-acid |
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PEG | 5 | Acid |
7568 | VH 032 amide-PEG6-amine |
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PEG | 6 | Amine |
6909 | VH 032 phenol-alkylC4-amine |
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Alkyl | 4 | Amine |
6910 | VH 032 phenol-alkylC6-amine |
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Alkyl | 6 | Amine |
7293 | VH 101 phenol-alkylC4-amine |
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Alkyl | 4 | Amine |
Cat. No. | Product Name | Structure | E3 Ligase Exit Vector | Linker
Type |
Number
of Units |
Conjugation
Functionality |
---|---|---|---|---|---|---|
7516 | Lenalidomide 4'-alkylC3-azide |
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- | alkyl | 3 | Azide |
7517 | Lenalidomide 4'-alkylC5-azide |
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- | alkyl | 5 | Azide |
7075 | Lenalidomide 4'-PEG1-amine |
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- | PEG | 1 | Amine |
7513 | Lenalidomide 4'-PEG1-azide |
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- | PEG | 1 | Azide |
7093 | Lenalidomide 4'-PEG2-amine |
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- | PEG | 2 | Amine |
7514 | Lenalidomide 4'-PEG2-azide |
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- | PEG | 2 | Azide |
7076 | Lenalidomide 4'-PEG3-amine |
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- | PEG | 3 | Amine |
7515 | Lenalidomide 4'-PEG3-azide |
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- | PEG | 3 | Azide |
7472 | Lenalidomide 5'-piperazine |
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Piperazine | - | - | Amine |
7473 | Lenalidomide 5'-piperazine-4-methylpiperidine |
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Piperazine | Methyl-piperidine | 1 | Amine |
6851 | Pomalidomide 4'-alkylC2-amine |
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- | Alkyl | 2 | Amine |
7439 | Pomalidomide 4'-alkylC2-azide |
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- | Alkyl | 2 | Azide |
7096 | Pomalidomide 4'-alkylC3-acid |
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- | Alkyl | 3 | Carboxylic Acid |
7205 | Pomalidomide 4'-alkylC3-amine |
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- | Alkyl | 3 | Amine |
7440 | Pomalidomide 4'-alkylC3-azide |
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- | Alkyl | 3 | Azide |
7209 | Pomalidomide 4'-alkylC4-acid |
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- | Alkyl | 4 | Carboxylic Acid |
7441 | Pomalidomide 4'-alkylC4-azide |
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- | Alkyl | 4 | Azide |
6682 | Pomalidomide 4'-alkylC5-acid |
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- | Alkyl | 5 | Carboxylic Acid |
6716 | Pomalidomide 4'-alkylC5-amine |
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- | Alkyl | 5 | Amine |
7442 | Pomalidomide 4'-alkylC5-azide |
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- | Alkyl | 5 | Azide |
7210 | Pomalidomide 4'-alkylC6-acid |
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- | Alkyl | 6 | Carboxylic Acid |
7923 | Pomalidomide 4'-alkylC6-amine |
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- | Alkyl | 6 | Amine |
7443 | Pomalidomide 4'-alkylC6-azide |
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- | Alkyl | 6 | Azide |
7097 | Pomalidomide 4'-alkylC7-acid |
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- | Alkyl | 7 | Carboxylic Acid |
7208 | Pomalidomide 4'-alkylC7-amine |
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- | Alkyl | 7 | Amine |
7211 | Pomalidomide 4'-alkylC8-acid |
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- | Alkyl | 8 | Carboxylic Acid |
6944 | Pomalidomide 4'-alkylC8-amine |
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- | Alkyl | 8 | Amine |
7732 | Pomalidomide 4'-alkylC10-amine |
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- | Alkyl | 10 | Amine |
7094 | Pomalidomide 4'-PEG1-acid |
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- | PEG | 1 | Acid |
7203 | Pomalidomide 4'-PEG1-amine |
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- | PEG | 1 | Ethylamine |
7434 | Pomalidomide 4'-PEG1-azide |
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- | PEG | 1 | Azide |
7212 | Pomalidomide 4'-PEG2-acid |
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- | PEG | 2 | Acid |
6637 | Pomalidomide 4'-PEG2-amine |
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- | PEG | 2 | Amine |
7307 | Pomalidomide 4'-PEG2-azide |
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- | PEG | 2 | Azide |
6681 | Pomalidomide 4'-PEG3-acid |
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- | PEG | 3 | Carboxylic Acid |
7204 | Pomalidomide 4'-PEG3-amine |
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- | PEG | 3 | Ethylamine |
7435 | Pomalidomide 4'-PEG3-azide |
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- | PEG | 3 | Azide |
7213 | Pomalidomide 4'-PEG4-acid |
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- | PEG | 4 | Acid |
6963 | Pomalidomide 4'-PEG4-amine |
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- | PEG | 4 | Ethylamine |
7436 | Pomalidomide 4'-PEG4-azide |
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- | PEG | 4 | Azide |
7095 | Pomalidomide 4'-PEG5-acid |
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- | PEG | 5 | Acid |
7437 | Pomalidomide 4'-PEG5-azide |
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- | PEG | 5 | Azide |
7438 | Pomalidomide 4'-PEG6-azide |
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- | PEG | 6 | Azide |
7468 | Pomalidomide 5'-piperazine |
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Piperazine | - | - | Amine |
7469 | Pomalidomide 5'-piperazine-4-methylpiperidine |
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Piperazine | Methyl-piperidine | 1 | Amine |
7470 | Pomalidomide 5'-fluoro-6-piperazine_7470 |
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Piperazine | - | - | Amine |
7471 | Pomalidomide 5'-fluoro-6-piperazine-4-methylpiperidine_7471 |
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Piperazine | Methyl-piperidine | 1 | Amine |
7329 | Thalidomide 4'-ether-alkylC2-acid |
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Alkyl | 2 | Acid |
6850 | Thalidomide 4'-ether-alkylC2-amine |
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Alkyl | 2 | Amine |
7330 | Thalidomide 4'-ether-alkylC3-acid |
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Alkyl | 3 | Acid |
7521 | Thalidomide 4'-ether-alkylC3-azide |
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Alkyl | 3 | Azide |
7331 | Thalidomide 4'-ether-alkylC4-acid |
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Alkyl | 4 | Acid |
6917 | Thalidomide 4'-ether-alkylC4-amine |
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Alkyl | 4 | Amine |
7332 | Thalidomide 4'-ether-alkylC5-acid |
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Alkyl | 5 | Acid |
7522 | Thalidomide 4'-ether-alkylC5-azide |
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Alkyl | 5 | Azide |
6627 | Thalidomide 4'-ether-alkylC6-amine |
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Alkyl | 6 | Amine |
7333 | Thalidomide 4'-ether-alkylC6-acid |
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Alkyl | 6 | Acid |
7334 | Thalidomide 4'-ether-alkylC7-acid |
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Alkyl | 7 | Acid |
7335 | Thalidomide 4'-ether-alkylC8-acid |
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Alkyl | 8 | Acid |
7403 | Thalidomide 4'-ether-alkylC8-amine |
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Alkyl | 8 | Amine |
7518 | Thalidomide 4'-ether-PEG1-azide |
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PEG | 1 | Azide |
6686 | Thalidomide 4'-ether-PEG2-alkyne |
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PEG | 2 | Alkyne |
7519 | Thalidomide 4'-ether-PEG2-azide |
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PEG | 2 | Azide |
6950 | Thalidomide 4'-ether-PEG3-amine |
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PEG | 3 | Ethylamine |
7520 | Thalidomide 4'-ether-PEG3-azide |
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PEG | 3 | Azide |
6951 | Thalidomide 4'-ether-PEG5-amine |
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PEG | 5 | Ethylamine |
6949 | Thalidomide 4'-oxyacetamide-alkylC2-amine |
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Alkyl | 2 | Amine |
6469 | Thalidomide 4'-oxyacetamide-alkylC4-amine |
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Alkyl | 4 | Amine |
6968 | Thalidomide 4'-oxyacetamide-alkylC6-amine |
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Alkyl | 6 | Amine |
6946 | Thalidomide 4'-oxyacetamide-alkylC8-amine |
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Alkyl | 2 | Amine |
6300 | Thalidomide 4'-oxyacetamide-alkylC4-azide |
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Alkyl | 4 | Azide |
6966 | Thalidomide 4'-oxyacetamide-PEG1-amine |
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PEG | 1 | Ethylamine |
6967 | Thalidomide 4'-oxyacetamide-PEG2-amine |
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PEG | 2 | Ethylamine |
6467 | Thalidomide 4'-oxyacetamide-PEG3-amine |
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PEG | 3 | Amine |
6468 | Thalidomide 4'-oxyacetamide-PEG4-amine |
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PEG | 4 | Amine |
6913 | Thalidomide 4'-oxyacetamide-alkylC1-PEG3-alkylC3-amine |
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Alkyl-PEG-Alkyl | 1-3-3 | Amine |
7557 | Thalidomide 5'-amine-alkylc8-amine |
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Alkyl | 8 | Ethylamine |
7733 | Thalidomide 5'-amine-alkylC10-amine |
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Alkyl | 10 | Ethylamine |
7735 | Thalidomide 5'-amine-PEG1-amine |
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alkyl | 10 | Ethylamine |
7736 | Thalidomide 5'-amine-PEG2-amine |
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PEG | 2 | Ethylamine |
7737 | Thalidomide 5'-amine-PEG3-amine |
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PEG | 3 | Ethylamine |
Cat. No. | Product Name | Structure | E3 Ligase Exit Vector | Linker
Type |
Number
of Units |
Conjugation
Functionality |
---|---|---|---|---|---|---|
6474 | A 410099.1 amide-alkylC4-amine |
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Amide-Alkyl | 4 | Amine |
6473 | A 410099.1 amide-PEG2-amine |
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Amide-PEG | 2 | Amine |
6472 | A 410099.1 amide-PEG3-amine |
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Amide-PEG | 3 | Amine |
7220 | A 410099.1 amide-PEG4-amine |
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Amide-PEG | 4 | Amine |
7221 | A 410099.1 amide-PEG5-amine |
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Amide-PEG | 5 | Amine |
Cat. No. | Product Name | Structure | E3 Ligase Ligand | Target E3 | Reactive Handle | Reaction Chemistry |
---|---|---|---|---|---|---|
6471 | A 410099.1, amine |
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A 410099.1 | IAP | Primary Amine | Amide coupling |
7178 | LCL 161, phenol |
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LCL 161 | IAP | Alcohol | Mitsunobu reaction |
7677 | Lenalidomide 5'-amine |
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Lenalidomide | Cereblon | Primary Amine | Amide Coupling |
7858 | PD 4'-oxyacetic acid |
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Phenyl Dihydrouracil | Cereblon | Carboxylic Acid | Amide Coupling |
7859 | PD 4'-piperazine |
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Phenyl Dihydrouracil | Cereblon | Cyclic Amine | Amide Coupling |
7670 | Phenyl-glutarimide 4'-oxyacetic acid |
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Phenyl-glutarimide | Cereblon | Carboxylic Acid | Amide Coupling |
6466 | TC E3 5031 |
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Thalidomide | Cereblon | Carboxylic acid | Amide coupling |
6628 | TC E3 5032 |
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Pomalidomide | Cereblon | Fluorine | Nucleophilic aromatic substitution |
7456 | Thalidomide, 5'-fluoro |
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Thalidomide | Cereblon | Fluoro | Nucleophilic aromatic substitution |
6685 | Thalidomide, propargyl |
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Thalidomide | Cereblon | Alkyne | Click chemistry |
6462 | VH 032, amine |
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VH 032 | VHL | Primary amine | Amide coupling |
6969 | cis VH 032, amine dihydrochloride |
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VH 032 | VHL | Primary amine | Amide coupling |
7634 | Me VH 032, amine |
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VH 032 | VHL | Primary amine | Amide coupling |
6911 | VH 032, phenol |
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VH 032 | VHL | Alcohol | Mitsunobu reaction |
6683 | VH 032, propargyl |
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VH 032 | VHL | Alkyne | Click chemistry |
7861 | VH 032, thiol |
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VH 032 | VHL | Thiol | Nucleophilic substitution |
6952 | VH 101, phenol |
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VH 101 | VHL | Alcohol | Mitsunobu reaction |
7884 | VH 101, thiol |
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VH 101 | VHL | Thiol | Nucleophilic substitution |
Cat. No. | Product Name | Structure | Ligand | Target Protein | Reactive Handle | Reaction Chemistry |
---|---|---|---|---|---|---|
7689 | (+)-JQ1 bump, acid functionalized |
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JQ1 analog | BET Bromodomains | Carboxylic acid | Amide coupling |
6588 | (+)-JQ1 carboxylic acid |
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JQ1 | BET Bromodomains | Carboxylic acid | Amide coupling |
7576 | (+)-JQ1 maleimide |
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JQ1 | BET Bromodomains | Maleimide | Sulfhydryl coupling |
6589 | (+)-JQ1 PA |
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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.
Tocris offers the following scientific literature for Degrader Building Blocks to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
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