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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.

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Related Categories

    VHL Targeting Ligands Plus Linkers

    Cat. No. Product Name Structure E3 Ligase Exit Vector Linker
    Type    		 Number
    of Units    		 Conjugation
    Functionality
    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
    7216 VH 032 amide-alkylC3-acid Cat.No. 7216 - VH 032 amide-alkylC3-acid Tools for Targeted Protein Degradation Alkyl 3 Acid
    7073 VH 032 amide-alkylC3-amine Cat.No. 7073 - VH 032 amide-alkylC3-amine Tools for Targeted Protein Degradation Alkyl 3 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
    7217 VH 032 amide-alkylC5-acid Cat.No. 7217 - VH 032 amide-alkylC5-acid Tools for Targeted Protein Degradation Alkyl 5 Acid
    6985 VH 032 amide-alkylC5-amine Cat.No. 6985 - VH 032 amide-alkylC5-amine Tools for Targeted Protein Degradation Alkyl 5 Amine
    7867 VH 032 amide-alkylC5-azide Cat.No. 6985 - VH 032 amide-alkylC5-azide Tools for Targeted Protein Degradation Alkyl 5 Azide
    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
    7925 VH 032 amide-alkylC7-acid Cat.No. 7925 - VH 032 amide-alkylC7-acid Tools for Targeted Protein Degradation Alkyl 7 Carboxylic Acid
    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
    7404 VH 032 amide-alkylC9-acid Cat.No. 7404 - VH 032 amide-alkylC9-acid Tools for Targeted Protein Degradation Alkyl 9 Carboxylic Acid
    7566 VH 032 amide-alkylC9-amine Cat.No. 7566 - VH 032 amide-alkylC9-amine Tools for Targeted Protein Degradation Alkyl 9 Amine
    6880 VH 032 amide-alkylC10-amine Cat.No. 6880 - VH 032 amide-alkylC10-amine Tools for Targeted Protein Degradation Alkyl 10 Amine
    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
    7215 VH 032 amide-PEG4-acid Cat.No. 7215 - VH 032 amide-PEG4-acid Tools for Targeted Protein Degradation PEG 4 Carboxylic Acid
    6464 VH 032 amide-PEG4-amine Cat.No. 6464 - VH 032 amide-PEG4-amine Tools for Targeted Protein Degradation PEG 4 Amine
    7105 VH 032 amide-PEG5-acid Cat.No. 7105 - VH 032 amide-PEG5-acid Tools for Targeted Protein Degradation PEG 5 Acid
    7568 VH 032 amide-PEG6-amine Cat.No. 7568 - VH 032 amide-PEG6-amine Tools for Targeted Protein Degradation PEG 6 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
    7516 Lenalidomide 4'-alkylC3-azide Cat.No. 7516 - Lenlidomide 4'-alkylC3-azide - alkyl 3 Azide
    7517 Lenalidomide 4'-alkylC5-azide Cat.No. 7517 - Lenlidomide 4'-alkylC5-azide - alkyl 5 Azide
    7075 Lenalidomide 4'-PEG1-amine Cat.No. 7075 - Lenlidomide 4'-PEG1-amine - PEG 1 Amine
    7513 Lenalidomide 4'-PEG1-azide Cat.No. 7513 - Lenlidomide 4'-PEG1-azide - PEG 1 Azide
    7093 Lenalidomide 4'-PEG2-amine Cat.No. 7093 - Lenlidomide 4'-PEG2-amine - PEG 2 Amine
    7514 Lenalidomide 4'-PEG2-azide Cat.No. 7514 - Lenlidomide 4'-PEG2-azide - PEG 2 Azide
    7076 Lenalidomide 4'-PEG3-amine Cat.No. 7076 - Lenlidomide 4'-PEG3-amine - PEG 3 Amine
    7515 Lenalidomide 4'-PEG3-azide Cat.No. 7515 - Lenlidomide 4'-PEG3-azide - PEG 3 Azide
    7472 Lenalidomide 5'-piperazine Cat.No. 7472 - Lenlidomide 5'-piperazine Piperazine - - Amine
    7473 Lenalidomide 5'-piperazine-4-methylpiperidine Cat.No. 7473 - Lenalidomide 5'-piperazine-4-methylpiperidine Piperazine Methyl-piperidine 1 Amine
    7998 PAG 4'-piperazine Cat.No. 7998 - PAG 4'-piperazine Piperazine - - Amine
    7999 PAG 4'-piperazine-4-methylpiperidine Cat.No. 7999 - PAG 4'-piperazine-4-methylpiperidine Piperazine Methyl-piperidine 1 Amine
    6851 Pomalidomide 4'-alkylC2-amine Cat.No. 6851 - Pomalidomide 4'-alkylC2-amine - Alkyl 2 Amine
    7439 Pomalidomide 4'-alkylC2-azide Cat.No. 7439 - Pomalidomide 4'-alkylC2-azide - Alkyl 2 Azide
    7096 Pomalidomide 4'-alkylC3-acid Cat.No. 7096 - Pomalidomide 4'-alkylC3-acid - Alkyl 3 Carboxylic Acid
    7205 Pomalidomide 4'-alkylC3-amine Cat.No. 7205 - Pomalidomide 4'-alkylC3-amine - Alkyl 3 Amine
    7440 Pomalidomide 4'-alkylC3-azide Cat.No. 7440 - Pomalidomide 4'-alkylC3-azide - Alkyl 3 Azide
    7209 Pomalidomide 4'-alkylC4-acid Cat.No. 7209 - Pomalidomide 4'-alkylC4-acid - Alkyl 4 Carboxylic Acid
    7441 Pomalidomide 4'-alkylC4-azide Cat.No. 7441 - Pomalidomide 4'-alkylC4-azide - Alkyl 4 Azide
    6682 Pomalidomide 4'-alkylC5-acid Cat.No. 6682 - Pomalidomide 4'-alkylC5-acid - Alkyl 5 Carboxylic Acid
    6716 Pomalidomide 4'-alkylC5-amine Cat.No. 6716 - Pomalidomide 4'-alkylC5-amine - Alkyl 5 Amine
    7442 Pomalidomide 4'-alkylC5-azide Cat.No. 7442 - Pomalidomide 4'-alkylC5-azide - Alkyl 5 Azide
    7210 Pomalidomide 4'-alkylC6-acid Cat.No. 7210 - Pomalidomide 4'-alkylC6-acid - Alkyl 6 Carboxylic Acid
    7923 Pomalidomide 4'-alkylC6-amine Cat.No. 7923 - Pomalidomide 4'-alkylC6-amine - Alkyl 6 Amine
    7443 Pomalidomide 4'-alkylC6-azide Cat.No. 7443 - Pomalidomide 4'-alkylC6-azide - Alkyl 6 Azide
    7097 Pomalidomide 4'-alkylC7-acid Cat.No. 7097 - Pomalidomide 4'-alkylC7-acid - Alkyl 7 Carboxylic Acid
    7208 Pomalidomide 4'-alkylC7-amine Cat.No. 7208 - Pomalidomide 4'-alkylC7-amine - Alkyl 7 Amine
    7211 Pomalidomide 4'-alkylC8-acid Cat.No. 7211 - Pomalidomide 4'-alkylC8-acid - Alkyl 8 Carboxylic Acid
    6944 Pomalidomide 4'-alkylC8-amine Cat.No. 6944 - Pomalidomide 4'-alkylC8-amine - Alkyl 8 Amine
    7732 Pomalidomide 4'-alkylC10-amine Cat.No. 7732 - Pomalidomide 4'-alkylC10-amine - Alkyl 10 Amine
    7094 Pomalidomide 4'-PEG1-acid Cat.No. 7094 - Pomalidomide 4'-PEG1-acid - PEG 1 Acid
    7203 Pomalidomide 4'-PEG1-amine Cat.No. 7203 - Pomalidomide 4'-PEG1-amine - PEG 1 Ethylamine
    7434 Pomalidomide 4'-PEG1-azide Cat.No. 7434 - Pomalidomide 4'-PEG1-azide - PEG 1 Azide
    7212 Pomalidomide 4'-PEG2-acid Cat.No. 7212 - Pomalidomide 4'-PEG2-acid - PEG 2 Acid
    6637 Pomalidomide 4'-PEG2-amine Cat.No. 6637 - Pomalidomide 4'-PEG2-amine - PEG 2 Amine
    7307 Pomalidomide 4'-PEG2-azide Cat.No. 7307 - Pomalidomide 4'-PEG2-azide - PEG 2 Azide
    6681 Pomalidomide 4'-PEG3-acid Cat.No. 6681 - Pomalidomide 4'-PEG3-acid - PEG 3 Carboxylic Acid
    7204 Pomalidomide 4'-PEG3-amine Cat.No. 7204 - Pomalidomide 4'-PEG3-amine - PEG 3 Ethylamine
    7435 Pomalidomide 4'-PEG3-azide Cat.No. 7435 - Pomalidomide 4'-PEG3-azide - PEG 3 Azide
    7213 Pomalidomide 4'-PEG4-acid Cat.No. 7213 - Pomalidomide 4'-PEG4-acid - PEG 4 Acid
    6963 Pomalidomide 4'-PEG4-amine Cat.No. 6963 - Pomalidomide 4'-PEG4-amine - PEG 4 Ethylamine
    7436 Pomalidomide 4'-PEG4-azide Cat.No. 7436 - Pomalidomide 4'-PEG4-azide - PEG 4 Azide
    7095 Pomalidomide 4'-PEG5-acid Cat.No. 7095 - Pomalidomide 4'-PEG5-acid - PEG 5 Acid
    7437 Pomalidomide 4'-PEG5-azide Cat.No. 7437 - Pomalidomide 4'-PEG5-azide - PEG 5 Azide
    7438 Pomalidomide 4'-PEG6-azide Cat.No. 7438 - Pomalidomide 4'-PEG6-azide - PEG 6 Azide
    7468 Pomalidomide 5'-piperazine Cat.No. 7468 - Pomalidomide 5'-piperazine Piperazine - - Amine
    7469 Pomalidomide 5'-piperazine-4-methylpiperidine Cat.No. 7469 - Pomalidomide 5'-piperazine-4-methylpiperidine Piperazine Methyl-piperidine 1 Amine
    7470 Pomalidomide 5'-fluoro-6-piperazine Cat.No. 7470 - Pomalidomide 5'-fluoro-6'-piperazine Piperazine - - Amine
    7471 Pomalidomide 5'-fluoro-6-piperazine-4-methylpiperidine Cat.No. 7471 - Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine Piperazine Methyl-piperidine 1 Amine
    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
    7521 Thalidomide 4'-ether-alkylC3-azide Cat.No. 7521 - Thalidomide 4'-ether-alkylC3-azide Tools for Targeted Protein Degradation Alkyl 3 Azide
    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
    7522 Thalidomide 4'-ether-alkylC5-azide Cat.No. 7522 - Thalidomide 4'-ether-alkylC5-azide Tools for Targeted Protein Degradation Alkyl 5 Azide
    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
    7829 Thalidomide 4'-ether-alkylC6-azide Cat.No. 7829 - Thalidomide 4'-ether-alkylC6-azide Tools for Targeted Protein Degradation Alkyl 6 Azide
    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
    7403 Thalidomide 4'-ether-alkylC8-amine Cat.No. 7403 - Thalidomide 4'-ether-alkylC8-amine Tools for Targeted Protein Degradation Alkyl 8 Amine
    7518 Thalidomide 4'-ether-PEG1-azide Cat.No. 7518 - Thalidomide 4'-ether-peg1-azide Tools for Targeted Protein Degradation PEG 1 Azide
    6686 Thalidomide 4'-ether-PEG2-alkyne Cat.No. 6686 - Thalidomide 4'-ether-PEG2-alkyne Tools for Targeted Protein Degradation PEG 2 Alkyne
    7519 Thalidomide 4'-ether-PEG2-azide Cat.No. 7519 - Thalidomide 4'-ether-PEG2-azide Tools for Targeted Protein Degradation PEG 2 Azide
    6950 Thalidomide 4'-ether-PEG3-amine Cat.No. 6850 - Thalidomide 4'-ether-PEG3-amine Tools for Targeted Protein Degradation PEG 3 Ethylamine
    7520 Thalidomide 4'-ether-PEG3-azide Cat.No. 7520 - Thalidomide 4'-ether-PEG3-azide Tools for Targeted Protein Degradation PEG 3 Azide
    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'-oxyacetamide-alkylC1-PEG3-alkylC3-amine Tools for Targeted Protein Degradation Alkyl-PEG-Alkyl 1-3-3 Amine
    7988 Thalidomide 5'-amine-alkylc6-amine Cat.No. 7988 - Thalidomide 5'-amine-alkylC6-amine Tools for Targeted Protein Degradation Alkyl 6 Ethylamine
    7557 Thalidomide 5'-amine-alkylc8-amine Cat.No. 7557 - Thalidomide 5'-amine-alkylC8-amine Tools for Targeted Protein Degradation Alkyl 8 Ethylamine
    7733 Thalidomide 5'-amine-alkylC10-amine Cat.No. 7733 - Thalidomide 5'-amine-alkylC10-amine Tools for Targeted Protein Degradation Alkyl 10 Ethylamine
    7735 Thalidomide 5'-amine-PEG1-amine Cat.No. 7735 - Thalidomide 5'-amine-PEG1-amine Tools for Targeted Protein Degradation alkyl 10 Ethylamine
    7736 Thalidomide 5'-amine-PEG2-amine Cat.No. 7736 - Thalidomide 5'-amine-PEG2-amine Tools for Targeted Protein Degradation PEG 2 Ethylamine
    7737 Thalidomide 5'-amine-PEG3-amine Cat.No. 7737 - Thalidomide 5'-amine-PEG3-amine Tools for Targeted Protein Degradation PEG 3 Ethylamine

    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
    8066 CST 530, Phenol Cat.No. 8066 - CST 530, Phenol CST 530 IAP Alcohol Mitsunobu reaction
    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
    7677 Lenalidomide 5'-amine Cat.No. 7677 - Lenalidomide 5'-amine Lenalidomide Cereblon Primary Amine Amide Coupling
    7858 PD 4'-oxyacetic acid Cat.No. 7858 - PD 4'-oxyacetic acid Phenyl Dihydrouracil Cereblon Carboxylic Acid Amide Coupling
    7859 PD 4'-piperazine Cat.No. 7859 - PD 4'-piperazine Phenyl Dihydrouracil Cereblon Cyclic Amine Amide Coupling
    7670 Phenyl-glutarimide 4'-oxyacetic acid Cat.No. 7670 - Phenyl-glutarimide 4'-oxyacetic acid Phenyl-glutarimide Cereblon Carboxylic Acid Amide Coupling
    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
    7456 Thalidomide, 5'-fluoro Cat. No. 7456 - Thalidomide, 5'-fluoro Thalidomide Cereblon Fluoro 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
    7634 Me VH 032, amine Cat. No. 7634 - Me VH 032, amine 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
    7861 VH 032, thiol Cat. No. 7861 - VH 032, thiol VH 032 VHL Thiol Nucleophilic substitution
    6952 VH 101, phenol Cat. No. 6952 - VH 101, phenol VH 101 VHL Alcohol Mitsunobu reaction
    7884 VH 101, thiol Cat. No. 7884 - VH 101, thiol VH 101 VHL Thiol Nucleophilic substitution

    Functionalized Warhead Ligands

    Cat. No. Product Name Structure Ligand Target Protein Reactive Handle Reaction Chemistry
    7689 (+)-JQ1 bump, acid functionalized Cat. No. 7689 - (+)-JQ1 bump, acid functionalized JQ1 analog BET Bromodomains Carboxylic acid Amide coupling
    6588 (+)-JQ1 carboxylic acid Cat. No. 6588 - (+)-JQ1 carboxylic acid JQ1 BET Bromodomains Carboxylic acid Amide coupling
    7576 (+)-JQ1 maleimide Cat. No. 7576 - (+)-JQ1 maleimide JQ1 BET Bromodomains Maleimide Sulfhydryl 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* your copy today!

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

    TPD and Induced Proximity Research Product Guide

    TPD and Induced Proximity Research Product Guide

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

    • Active Degraders
    • TAG Degradation Platform
    • Degrader Building Blocks
    • Assays for Protein Degradation
    • Induced Proximity Tools
    Developing Degraders Poster

    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 Poster

    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 Poster

    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