Protein Degraders

Protein Degraders (e.g.PROTAC® molecules, SNIPERs etc), are a new approach for the knockdown of target proteins within cells. Comprising binding moieties for an E3 ubiquitin ligase and a target protein joined by a linker, these hybrid molecules induce selective, proteasome-dependent degradation of target proteins and can be used to investigate downstream effects of protein knockdown or to interfere with specific signaling pathways.

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

Literature (4)


Cat. No. Product Name / Activity
8040 α-Synuclein Degrader 2b
α-synuclein Degrader (PROTAC®)
7278 α1A-AR Degrader 9c
Selective α1A adrenergic receptor Degrader (PROTAC®)
7254 ARCC 4
Potent and selective androgen receptor PROTAC®
7256 ARV 771
Potent BET bromodomain PROTAC®; also degrades BRD-tagged chimeric antigen receptors (CAR) in T cells
6356 AT 1
(+)-JQ1 based PROTAC® with selectivity for BRD4
7699 AUTAC4
Mitochondrial targeting AUTAC Degrader
Photoswitchable BET bromodomain Degrader (PHOTAC)
6921 BSJ-03-123
Selective Cdk6 Degrader (PROTAC®)
6938 BSJ-03-204
Selective Cdk4/6 Degrader (PROTAC®)
6937 BSJ-04-132
Selective Cdk4 Degrader (PROTAC®)
7528 BSJ-4-116
Selective CDK12 PROTAC® Degrader
7425 CG 428
Potent tropomyosin receptor kinase (TRK) degrader
7427 CG 858
Selective BRAF-V600E protein Degrader (uSMITE™)
6416 CM 11
Homo-PROTAC® for self-degradation of pVHL30
7800 CPS2
Potent and selective CDK2 Degrader (PROTAC®)
7219 CRBN PROTAC® 14a
Cereblon Degrader (PROTAC®)
6948 CRBN-6-5-5-VHL
Potent and selective cereblon Degrader (PROTAC®); cell-permeable
8021 CST 626
Potent pan IAP Degrader (PROTAC®)
7745 CST 905
Potent and selective BRAFV600E Degrader (PROTAC®)
7801 CST 967
Potent and selective USP7 Degrader (PROTAC®)
6327 dBET1
(+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
6945 dBET6
Potent and selective (+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
6606 dBRD9
Potent and selective BRD9 Degrader (PROTAC®)
6943 dBRD9-A
Potent BRD9 Degrader (PROTAC®)
7160 DD 03-171
Potent and selective BTK Degrader (PROTAC®)
6607 dTRIM 24
TRIM24 Degrader (PROTAC®)
7306 FC 11
Highly potent focal adhesion kinase (FAK) Degrader (PROTAC®)
7258 Gefitinib-based PROTAC® 3
7265 GMB 475
7818 GSK 215
Potent and selective focal adhesion kinase (FAK) Degrader (PROTAC®)
7882 HDAC4 CHDI Degrader 11
Potent and selective HDAC4 Degrader (PROTAC®)
Potent and selective HER2 targeting Degrader (PROTAC®)
7828 HHP 9
BET bromodomain Degrader (PROTAC®); also potent Hedgehog pathway inhibitor
7983 IRAK3 Degrader 23
IRAK3 PROTAC® Degrader
7837 JB 300
Aurora A Degrader (PROTAC®)
7304 JH-XI-10-02
CDK8 Degrader (PROTAC®)
8029 JNJ 1013
Interleukin 1 Receptor Associated Kinase 1 (IRAK1) Degrader (PROTAC®)
7682 JQAD1
Potent and selective EP300 Degrader (PROTAC®)
7420 LC 2
Selective KRAS Degrader (PROTAC®)
7813 LL-K9-3
Selective HyT-based degrader of the CDK9-cyclin T1 complex
7503 MD13
Potent MIF Degrader (PROTAC®)
7395 MS 154
Potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant EGFR
7397 MS 39
Potent and selective VHL-recruiting Degrader (PROTAC®) of mutant EGFR
6154 MZ 1
(+)-JQ1 based Degrader (PROTAC®) that preferentially degrades BRD4
Potent and selective nicotinamide phosphoribosyl transferase (NAMPT) Degrader (PROTAC®)
7388 ND1-YL2
SRC-1 peptide-based Degrader (PROTAC®); active in vivo
7177 NR 7h
Potent and selective p38α and p38β Degrader (PROTAC®); active in vivo
8004 PROTAC®(H-PGDS)-7
Potent hematopoietic prostaglandin D2 synthase Degrader (PROTAC®)
7651 PT-65
Potent GSK3 Degrader (PROTAC®)
7432 SIM1
Potent and selective trivalent BET Bromodomain Degrader (PROTAC®)
7675 SJ 1008030
Selective JAK2 Degrader (PROTAC®)
7727 SJ 10542
Potent and selective JAK2/3 Degrader (PROTAC®)
7721 SJ 11646
Potent and selective LCK Degrader (PROTAC®)
7463 SJF 0628
7261 SJF 1521
Selective EGFR PROTAC®
7262 SJF 1528
Potent EGFR PROTAC®; also degrades HER2
7266 SJF 8240
c-MET PROTAC®; also degrades exon-14-deleted c-MET
7268 SJFα
Potent and selective p38α PROTAC®
7267 SJFδ
Potent and selective p38δ PROTAC®
7583 SK 575
Potent PARP1 Degrader (PROTAC®)
7120 SNIPER(ER)-87
Potent and selective ERα Degrader (SNIPER)
8053 STING Degrader SP23
Selective STING Degrader (PROTAC®)
7259 TBK1 PROTAC® 3i
Potent TANK-binding kinase 1 (TBK1) PROTAC®
6532 THAL SNS 032
Potent and selective Cdk9 Degrader (PROTAC®)
6524 TL 12-186
Multikinase Degrader (PROTAC®)
6745 TL 13-112
Selective ALK Degrader (PROTAC®)
6744 TL 13-12
Selective ALK Degrader (PROTAC®)
7816 UNC 6852
Polycomb repressive complex 2 (PRC2) Degrader PROTAC®
6936 VZ 185
Potent and selective BRD7/9 Degrader (PROTAC®)
7298 xStAx-VHLL
Selective peptide-based β-catenin Degrader (PROTAC®)
7240 ZNL 02-096
Potent and selective Wee1 Degrader (PROTAC®)


Cat. No. Product Name / Activity
8041 α-Synuclein Degrader 2bn
Negative control for α Synuclein Degrader 2b (Cat. No. 8040)
7255 ARCC 4 negative control
Negative control for ARCC 4 (Cat. No. 7254)
7529 BSJ-4-116-NC
Negative control for BSJ-4-116 (Cat. No. 7528).
6922 BSJ-Bump
Negative control for BSJ-03-123 (Cat. No. 6921)
7426 CG 428-Neg
Negative control for CG 428 (Cat. No. 7425)
7428 CG 858-Neg
Negative control for CG 858 (Cat. No. 7427)
6155 cis MZ 1
Negative Control for MZ 1 (Cat. No. 6154)
7433 cis-SIM1
Negative control for SIM1 (Cat. No. 7432)
6939 cis-VZ 185
Negative control for VZ 185 (Cat. No. 6936)
7421 LC 2 Epimer
Negative control for LC 2 (Cat. No. 7420)
7504 MD15
Negative control for MD13 (Cat. No. 7503)
7396 MS 154N
Negative control for MS 154 (Cat No. 7395)
7398 MS 39N
Negative control for MS 39 (Cat. No. 7397)
8005 PROTAC®(H-PGDS)-8
Negative control for PROTAC®(H-PGDS)-7 (Cat. No. 8004)
7464 SJF 0661
Negative control for SJF 0628 (Cat. No. 7463)
7588 SK 575-NEG
Negative control for SK 575 (Cat. No. 7583)
8054 STING Degrader N-Me-SP23
Negative control for STING Degrader SP23 (Cat. No. 8053)
7260 TBK1 control PROTAC® 4
Negative control for TBK1 PROTAC® 3i (Cat. No. 7259)
6746 TL 13-110
Negative control for TL 13-112 (Cat. No. 6745)
6747 TL 13-22
Negative control for TL 13-12 (Cat. No. 6744)
6525 TL 13-27
Negative control for TL 12-186 (Cat. No. 6524)

Protein Degraders (e.g.PROTAC® molecules, SNIPERs etc), are a useful approach for the knockdown of target proteins within cells. Comprising binding moieties for an E3 ubiquitin ligase and a target protein joined by a linker, these hybrid molecules induce selective, proteasome-dependent degradation of target proteins and can be used to investigate downstream effects of protein knockdown or to interfere with specific signaling pathways. The methodology provides an attractive alternative to RNAi methods and have several advantages including:

  • Ease of use: protein Degraders are cell permeable small molecules that can be applied directly to cells with no need for expression vectors or transfection
  • The duration of effect is adjustable and can be reversed on compound washout
  • Broad applicability to different cell lines, small molecule Degraders do not require cells that are easily transfectable
  • Catalytic mode of action: they dissociate following ubiquitination and rebind to new target proteins, which allows their use at sub-stoichiometric concentrations.

Protein Degraders - Tools for Targeted Protein Degradation

Active Degraders - Tools for Targeted Protein Degradation

Figure 1: Schematic showing the catalytic mode of action of heterobifunctional degrader molecules. Degraders initiate the formation of a ternary complex between an E3 ubiquitin ligase and a target protein which results in polyubiquitination of the target protein, its recognition by the proteasome and subsequent degradation. Degraders act catalytically by repeatedly engaging and directing the ubiquitination of target molecules.

Adapted from Tinworth et al. (2016) MedChemComm 7 2206.

Another interesting feature of small molecule Degraders is their ability to confer additional selectivity, compared to the profile of the target protein ligand used. This is exemplified by AT 1 (Cat. No. 6356), which selectively degrades BRD4, whereas the target protein ligand component of AT 1, (+)- JQ1 (Cat. No. 4499), inhibits the closely related bromodomains of multiple BET family proteins.

Degraders are pharmacologically characterized by their DC50 and DMax values. These values can be used as a guide for the appropriate starting concentrations to use for your experiment. The DC50 is analogous to traditional IC50 values and is the concentration of Degrader at which 50% of the target protein is degraded. The DMax is the maximum level of degradation achievable.

An important factor to consider when using these products is the timescale required for maximum efficacy. This depends on the individual Degrader used; customers are referred to the references provided for each product for guidance. Another consideration is the 'hook effect', which leads to reduced degradation efficiency when high concentrations of compound are applied to cells. This is due to the formation of binary complexes, that compete with formation of the ternary complexes (E3 ligase-Degrader-target protein) required to achieve degradation. In general, very low concentrations of Degrader are required to achieve effective knock down.

Literature for Protein Degraders

Tocris offers the following scientific literature for Protein Degraders 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.

Targeted Protein Degradation Research Product Guide

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
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

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