TC-E3 5032

Name: TC-E3 5032
Brand: BOC Sciences
Price: 439 USD
Availability: MadeToOrder

CAS No.: 835616-60-9

Cat No.: BP-200006

Purity: ≥ 98% 4.5

TC-E3 5032 is a high-affinity ligand for E3 ligase, specifically optimized for use in PROTAC (Proteolysis Targeting Chimera) research and targeted protein degradation studies. As an E3 Ligase Ligand, TC-E3 5032 serves as a crucial building block for the design of bifunctional molecules that bring together a target protein and the cellular ubiquitin-proteasome system, leading to selective protein degradation. With well-characterized E3 ligase binding properties, TC-E3 5032 is widely utilized in the development of next-generation therapeutics and functional genomics research. This compound enables researchers to efficiently explore new degrader strategies and protein targets, advancing the field of targeted protein degradation and drug discovery.

Structure of 835616-60-9

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Category

Ligand for E3 Ligase

Molecular Formula

C13H9FN2O4

Molecular Weight

276.22

Appearance

White to Off-white Solid to Pale Purple Solid

* For research and manufacturing use only. Not for human or clinical use.

Size	Price	Stock	Quantity
5 g	$439	In stock

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Capabilities & Facilities

Comprehensive PROTAC Platform
Scientific Expertise & Technical Support
Custom Synthesis & Design Service
Extensive Product Coverage

Cutting-Edge Innovation
Fast Delivery & Global Support
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100% quality assurance

Popular Publications Citing BOC Sciences Products

Purity

≥ 98%

Solubility

Slightly soluble in Dichloromethane (Heated), DMSO

Appearance

White to Off-white Solid to Pale Purple Solid

ShelfLife

2 years

Storage

-20 °C

IUPACName

2-(2,6-dioxopiperidin-3-yl)-4-fluoroisoindole-1,3-dione

Synonyms

E3 ligase Ligand 4; 1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-fluoro-; Thalidomide 4-fluoride; Thalidomide fluoride; 4-Fluoro-thalidomide; Cereblon ligand 4;E3 ligase Ligand 4; 2-(2,6-Dioxo-3-piperidinyl)-4-fluoro-1H-isoindole-1,3(2H)-dione

Boiling Point

520.9±45.0 °C (Predicted)

Melting Point

254-256 °C

Density

1.570±0.06 g/cm3 (Predicted)

InChI Key

CRAUTELYXAAAPW-UHFFFAOYSA-N

InChI

InChI=1S/C13H9FN2O4/c14-7-3-1-2-6-10(7)13(20)16(12(6)19)8-4-5-9(17)15-11(8)18/h1-3,8H,4-5H2,(H,15,17,18)

SMILES

C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)F

Background Introduction

TC-E3 5032 is a synthetic ligand specifically designed for the recruitment of the Von Hippel-Lindau (VHL) E3 ubiquitin ligase complex. VHL ligands play a crucial role in targeted protein degradation strategies, such as PROTAC (Proteolysis Targeting Chimera) technology, by mediating substrate recognition and enabling the ubiquitin-proteasome system to selectively eliminate disease-associated proteins. TC-E3 5032 is engineered with a functional linker attachment site to facilitate the efficient development of novel PROTAC molecules.

Mechanism

TC-E3 5032 binds with high affinity to the VHL E3 ligase, mimicking the natural interaction between VHL and its endogenous substrates. Upon binding, TC-E3 5032 allows for the recruitment of the VHL E3 ligase complex to a target protein when covalently linked to a ligand specific for the protein of interest. This interaction forms a ternary complex, leading to target protein ubiquitination and subsequent proteasomal degradation. The design of TC-E3 5032 ensures optimal orientation and stability for effective PROTAC assembly and function.

Applications

TC-E3 5032 serves as a foundational building block for VHL-based PROTAC development and targeted protein degradation research. Its versatile structure supports conjugation with various ligands and linkers, enabling the synthesis of bifunctional degrader molecules. Common applications include:

• Generation of VHL-targeted PROTACs for functional genomics, drug discovery, and therapeutic development
• Construction of chemical tools to study protein function and validate new drug targets
• SAR optimization in the design of next-generation protein degraders
• Application in academic and CRO settings for custom degrader synthesis and mechanism-of-action studies.

• High-purity compound verified by HPLC, NMR, and LC-MS
• Consistent batch-to-batch reproducibility with complete QC documentation
• Supplied with COA, MSDS, and analytical data for traceability
• Reliable global shipping with stability-guaranteed packaging
• Dedicated technical support and optional custom synthesis service
• Demonstrates strong binding affinity to CRBN, VHL, or other E3 ligases
• Enables stable E3 ligase recruitment for targeted protein degradation
• Potent and selective ligand for E3 ligase recruitment, facilitating efficient target protein ubiquitination.
• Optimized structure for seamless incorporation into diverse PROTAC molecules, enabling robust targeted protein degradation assays.

1. Microenvironment in subchondral bone: predominant regulator for the treatment of osteoarthritis

Wenhui Hu, Shiwu Dong, Yueqi Chen, Ce Dou Ann Rheum Dis . 2021 Apr;80(4):413-422. doi: 10.1136/annrheumdis-2020-218089.

Osteoarthritis (OA) is a degenerative joint disease in the elderly. Although OA has been considered as primarily a disease of the articular cartilage, the participation of subchondral bone in the pathogenesis of OA has attracted increasing attention. This review summarises the microstructural and histopathological changes in subchondral bone during OA progression that are due, at the cellular level, to changes in the interactions among osteocytes, osteoblasts, osteoclasts (OCs), endothelial cells and sensory neurons. Therefore, we focus on how pathological cellular interactions in the subchondral bone microenvironment promote subchondral bone destruction at different stages of OA progression. In addition, the limited amount of research on the communication between OCs in subchondral bone and chondrocytes (CCs) in articular cartilage during OA progression is reviewed. We propose the concept of 'OC-CC crosstalk' and describe the various pathways by which the two cell types might interact. Based on the 'OC-CC crosstalk', we elaborate potential therapeutic strategies for the treatment of OA, including restoring abnormal subchondral bone remodelling and blocking the bridge-subchondral type H vessels. Finally, the review summarises the current understanding of how the subchondral bone microenvironment is related to OA pain and describes potential interventions to reduce OA pain by targeting the subchondral bone microenvironment.

2. Human NLRP1: From the shadows to center stage

Veit Hornung, Stefan Bauernfried J Exp Med . 2022 Jan 3;219(1):e20211405. doi: 10.1084/jem.20211405.

In response to infection or cell damage, inflammasomes form intracellular multimeric protein complexes that play an essential role in host defense. Activation results in the maturation and subsequent secretion of pro-inflammatory cytokines of the IL-1 family and a specific cell death coined pyroptosis. Human NLRP1 was the first inflammasome-forming sensor identified at the beginning of the millennium. However, its functional relevance and its mechanism of activation have remained obscure for many years. Recent discoveries in the NLRP1 field have propelled our understanding of the functional relevance and molecular mode of action of this unique inflammasome sensor, which we will discuss in this perspective.

3. Tuberculous bronchopleural fistula

Sarah C Boyd, Alexandra G A Stewart Respirol Case Rep . 2021 Mar 15;9(4):e00740. doi: 10.1002/rcr2.740.

Tuberculous bronchopleural fistula is a rare complication of pulmonary tuberculosis with presentation ranging from patients who are asymptomatic with incidental findings on imaging to those who present with acute tension pneumothorax.

Hello! What applications is TC-E3 5032 suitable for, please?

TC-E3 5032 is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. It can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966).

28/9/2017

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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂