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E3 Ligase Ligands

E3 ligase ligands bind ubiquitin ligases such as cereblon and von Hippel-Lindau (VHL) in degrader design. In a degrader, they anchor the ligase end of the molecule. E3 ubiquitin ligases transfer ubiquitin to substrate proteins and mark them for degradation by the proteasome. Thalidomide and its analogs bind cereblon (CRBN), a substrate receptor of a cullin-based E3 ligase complex identified as their direct target in 2010. The category includes cereblon ligands such as thalidomide fluoride and TD-106, and VHL ligands such as VL285 and VH032-cyclopropane-F. These ligands are used to build proteolysis-targeting chimeras (PROTACs) and to study how ligases are recruited to new substrates.

Cat. No.

A80592

CAS No.

3033591-48-6

E3 ligase Ligand 46

E3 Ligase Ligand 46 is a potent ligand that targets E3 ligases, facilitating the development of targeted protein degradation strategies. It is specifically utilized in the synthesis of PROTAC SMARCA2/4 degrader-36, enabling the selective degradation of cellular proteins. This compound offers valuable insights into the role of E3 ligases in cellular signaling and protein homeostasis, making it essential for research in targeted therapeutics and protein regulation.

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Cat. No.

A80593

CAS No.

2753651-18-0

E3 ligase Ligand 42

E3 ligase Ligand 42 is an E3 ubiquitin ligase ligand designed for targeted protein degradation applications. It can be conjugated to a target protein ligand via a linker, facilitating the synthesis of PROTAC AR Degrader-6. This compound effectively induces ubiquitination and subsequent degradation of proteins associated with cancer progression, making it a valuable tool for research in cancer biology and therapeutic development.

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Cat. No.

A80594

CAS No.

1466558-44-0

E3 ligase Ligand 68

E3 Ligase Ligand 68 is an E3 ligase ligand utilized in the development of PROTAC (proteolysis-targeting chimeras) molecules. It facilitates targeted protein degradation by enabling the conjugation of an E3 ligase to a ligand that binds the protein of interest. This reagent is essential for research applications aimed at studying protein homeostasis, disease mechanisms, and therapeutic interventions involving targeted protein degradation.

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Cat. No.

A80595

CAS No.

2758867-71-7

SJ1008066

SJ1008066 is an inhibitor of the MAGE-A11 protein, demonstrating an IC50 of 0.13 μM. It specifically binds to the MAGE homology domain (MHD), effectively disrupting the interaction between MAGE-A11 and PCF11. This mechanism presents valuable opportunities for research into cancer biology and therapeutic strategies targeting MAGE-A11 associated pathways.

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Cat. No.

A80596

CAS No.

2377849-57-3

E3 ligase Ligand 22

E3 Ligase Ligand 22 is a cereblon binder that facilitates the targeted degradation of Ikaros and Aiolos proteins through the ubiquitin-proteasome pathway. This compound is valuable for studies investigating protein homeostasis, immune regulation, and the mechanism of action of immunomodulatory drugs. Its selective interaction with cereblon makes it a useful tool for researchers exploring targeted protein degradation strategies in various biological contexts.

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Cat. No.

A80597

CAS No.

1948273-05-9

(R,S,S)-VH032-Me

(R,S,S)-VH032-Me is a ligand for E3 ubiquitin ligase, playing a crucial role in targeted protein degradation through the ubiquitin-proteasome pathway. It can be conjugated to proteins via a linker to create PROTACs such as dTAGV-1-NEG, which facilitate the selective degradation of oncogenic proteins. This compound is essential for studies involving targeted protein degradation, offering valuable insights into cancer biology and therapeutic development.

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25 mg

$290.00

50 mg

$420.00

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Cat. No.

A80598

CAS No.

1547163-02-9

Pomalidomide-5-O-CH3

Pomalidomide-5-O-CH3 is a synthetic derivative of Pomalidomide designed as a ligand for cereblon (CRBN), an E3 ubiquitin ligase. This compound facilitates the recruitment of CRBN, enabling targeted protein degradation through PROTAC (proteolysis targeting chimeras) technology. Pomalidomide-5-O-CH3 is valuable for research in targeted therapy and ubiquitin-proteasome system studies, contributing to insights in cancer treatment and cellular regulation.

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25 mg

$1,275.00

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Cat. No.

A80599

CAS No.

1005275-19-3

KLHDC2-IN-1

KLHDC2-IN-1 is a ligand that specifically targets the ubiquitin E3 ligase KLHDC2, exhibiting a dissociation constant (Kd) of 160 nM. This compound facilitates the development of PROTACs, which are designed to induce degradation of BRD4 in cellular environments. Its application in cellular research underscores its potential utility in studying protein degradation mechanisms and therapeutic strategies targeting BRD4-related pathways.

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Cat. No.

A80600

CAS No.

1799506-32-3

E3 ligase Ligand 58

E3 ligase Ligand 58 is a selective ligand for E3 ligases, facilitating the synthesis of proteolysis-targeting chimeras (PROTACs). This compound plays a critical role in targeted protein degradation, enabling researchers to explore cellular mechanisms and therapeutic applications. E3 ligase Ligand 58 serves as a valuable tool in drug development and biological research focused on post-translational modifications.

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Cat. No.

A80601

CAS No.

2488660-12-2

DA-PROTAC

DA-PROTAC is a selective PROTAC degrader targeting the copper ion-transport proteins Atox1 and CCS. By facilitating the recruitment of E3 ligase, DA-PROTAC promotes the ubiquitination and subsequent proteasomal degradation of both Atox1 and CCS. This compound is particularly valuable for research in triple negative breast cancer, allowing for the investigation of copper transport mechanisms and their implications in tumor biology.

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Cat. No.

A80602

CAS No.

1958262-04-8

CYCA-117-70

CYCA-117-70 is a ligand for DCAF1, exhibiting a binding affinity (KD) of 70 μM. It serves as an effective chemical handle for the development of proteolysis-targeting chimeras (PROTACs) that recruit DCAF1. This compound is valuable in research aiming to modulate protein degradation pathways, providing insights into cellular regulation and potential therapeutic applications.

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Cat. No.

A80604

CAS No.

3050687-80-1

CRBN ligand-17

CRBN ligand-17 is an E3 ubiquitin ligase ligand that targets the cereblon (CRBN) substrate recognition domain. This compound is essential for the design and synthesis of PROTACs (proteolysis-targeting chimeras), which facilitate targeted protein degradation. Its application in research includes studying protein regulation mechanisms and investigating therapeutic strategies for various diseases.

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Cat. No.

A80606

CAS No.

1061605-49-9

Deoxy-thalidomide-OMe

Deoxy-thalidomide-OMe is an E3 ligase ligand that plays a crucial role in targeted protein degradation mechanisms. This compound is utilized in the synthesis of PROTAC LRRK2 Degrader-4, facilitating research in the modulation of LRRK2 activity, which has implications in neurodegenerative diseases. Its ability to selectively engage with E3 ligases makes it a valuable tool for advancing studies in protein homeostasis and therapeutic development.

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Cat. No.

A80607

CAS No.

2489876-59-5

(S,R,R)-VH032

(S,R,R)-VH032 is a selective VHL ligand that facilitates targeted protein degradation through its interaction with the von Hippel-Lindau (VHL) E3 ubiquitin ligase complex. This compound serves as a crucial building block in the synthesis of PROTACs, specifically enabling the development of NCOA4 degrader-1. Its application in research highlights its potential for advancing studies in targeted protein degradation and therapeutic intervention strategies.

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Cat. No.

A80608

CAS No.

2355276-57-0

N-Demethylonalespib

N-Demethylonalespib is an effective ligand for E3 ligase, playing a crucial role in ubiquitination pathways. This compound is instrumental in the synthesis of DDO3602, facilitating research into protein degradation and cellular regulation. Its application in cellular biology makes it a valuable tool for investigating E3 ligase-targeted therapies.

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Cat. No.

A80609

CAS No.

2649154-64-1

RA183

RA183 is a selective ligand for E3 ligases, facilitating the development of proteolysis-targeting chimeras (PROTACs). This compound enables the targeted degradation of specific proteins by harnessing the ubiquitin-proteasome system, making it a valuable tool in chemical biology and drug discovery. RA183 can be utilized in various research applications aimed at elucidating protein function and developing innovative therapeutic strategies.

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Cat. No.

A80610

CAS No.

2641319-58-4

(S,R,S)-AHPC-Ala

(S,R,S)-AHPC-Ala is a ligand for E3 ubiquitin ligases, facilitating targeted protein degradation via the ubiquitin-proteasome pathway. This compound is instrumental in the synthesis of PROTAC SMARCA2/4-degrader-23, which is utilized in studies focused on the modulation of the SMARCA2 and SMARCA4 proteins. Its applications encompass research in cancer biology and therapeutic development, contributing to the advancement of targeted therapies.

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Cat. No.

A80611

CAS No.

105151-62-0

Arg12

Arg12 is a 12-amino acid peptide sequence that functions as a ligand for E3 ubiquitin ligases. This compound is valuable for the synthesis of PROTACs, including the PROTAC PLK1 Degrader-2. Additionally, Arg12 possesses cell-penetrating properties, enabling effective delivery of larger molecules into cells, making it a useful tool in cellular research and therapeutic applications.

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Cat. No.

A80612

CAS No.

790652-68-5

Lenalidomide-4-aminomethyl

Lenalidomide-4-aminomethyl is an E3 ligase ligand that specifically targets cereblon (CRBN), facilitating the recruitment of CRBN protein. This compound serves as an essential building block for the development of PROTAC molecules, enabling targeted protein degradation research. Its unique structural features make it a valuable tool for studying CRBN-mediated pathways and exploring therapeutic applications in cancer and other diseases.

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25 mg

$1,275.00

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Cat. No.

A80613

CAS No.

2154342-57-9

Pomalidomide-piperazine

Pomalidomide-piperazine is an active compound that serves as a critical building block for the synthesis of E3 ligands utilized in PROTAC (Proteolysis Targeting Chimeras) development. This compound facilitates targeted protein degradation by linking a protein of interest to an E3 ubiquitin ligase, promoting a novel approach to protein modulation. Its application is significant in drug discovery and therapeutic research focused on precision medicine.

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1 mg

$45.00

5 mg

$110.00

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Cat. No.

A80614

CAS No.

2357114-13-5

E3 ligase Ligand 31

E3 Ligase Ligand 31 is a specific ligand for E3 ubiquitin ligases, facilitating targeted protein degradation via the ubiquitin-proteasome system. This compound is instrumental in the synthesis of PTOTAC HSD17B13 degrader 1, making it a valuable tool for research in protein homeostasis and related therapeutic applications. Its utility in studying E3 ligase interactions offers insights into the modulation of protein levels in cellular and biochemical contexts.

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Cat. No.

A80615

CAS No.

2502205-74-3

Cyclopropane-(S,R,S)-AHPC

Cyclopropane-(S,R,S)-AHPC is a selective ligand for E3 ubiquitin ligases, which play a crucial role in ubiquitination processes affecting protein degradation and cellular regulation. This compound is valuable for research into post-translational modifications and protein interactions, enabling studies into cellular signaling pathways and disease mechanisms. Its ability to modulate E3 ligase activity makes it an essential tool for understanding protein homeostasis and developing targeted therapies.

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Cat. No.

A80616

CAS No.

2505504-49-2

E3 ligase Ligand 44

E3 Ligase Ligand 44 serves as an effective ligand for E3 ligases, facilitating the development of proteolysis-targeting chimeras (PROTACs) such as the AR Degrader-7. Its primary mechanism involves engaging E3 ligases to promote targeted protein degradation, enabling precise modulation of cellular pathways. This compound is useful in research focused on protein homeostasis, targeted therapy, and the exploration of novel therapeutic strategies in cancer and other diseases.

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Cat. No.

A80617

CAS No.

3034204-25-3

E3 ligase Ligand 27

E3 ligase Ligand 27 is a selective ligand targeting E3 ubiquitin ligases, facilitating the development of targeted protein degradation technologies. This compound is primarily utilized in the synthesis of the PROTAC BcI-2/BcI-xI Degrader-1, promoting the degradation of specific oncogenic proteins. Its application in research supports the investigation of novel therapeutic strategies in cancer treatment through the modulation of protein homeostasis.

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Cat. No.

A80618

CAS No.

1448189-66-9

VH032 analogue-2

VH032 analogue-2 is a selective ligand for the E3 ubiquitin ligase von Hippel-Lindau (VHL), facilitating its recruitment in cellular processes. This compound effectively removes its protective group under acidic conditions, enabling its direct utilization in the synthesis of PROTAC (Proteolysis Targeting Chimeras) molecules. VH032 analogue-2 serves as a crucial intermediate for the development of VHL-based PROTACs, making it a valuable tool for research in targeted protein degradation and related fields.

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