Functionalized E3 Ligase Ligands

Products
Literature (1)

Building Blocks

Cat. No. Product Name / Activity
6471 A 410099.1, amine
Functionalized IAP ligand for PROTACs
7678 5-Amino-Thalidomide
Cereblon ligand with amine on C5 for onward chemistry
7178 LCL 161, phenol
Functionalized IAP ligand for PROTACs
7670 Phenyl-glutarimide 4'-oxyacetic acid
Functionalized cereblon ligand for PROTAC development
7328 Photo-lenalidomide-acid
Functionalized photoswitchable cereblon ligand for Degraders
6628 TC E3 5032
Precursor to Pomalidomide-based PROTACs
7773 tDHU, acid
Functionalized cereblon ligand for PROTAC development
7456 Thalidomide, 5'-fluoro
Fluoro functionalized Thalidomide; cereblon ligand for PROTACs
6685 Thalidomide, propargyl
Alkyne-functionalized Thalidomide; 'click' cereblon ligand for PROTACs
6466 Thalidomide-4-hydroxyacetate
Carboxylic acid-functionalized Thalidomide; cereblon ligand for PROTACs
6462 VH 032, amine
Functionalized VHL ligand for PROTACs
6911 VH 032, phenol
Hydroxyl functionalized VHL ligand
6683 VH 032, propargyl
Alkyne-functionalized VH 032; 'click' VHL ligand for PROTACs
7758 VH 101, acid
VHL ligand, carboxylic acid functionalized at the benzylic position
6952 VH 101, phenol
Hydroxyl functionalized VHL ligand

Controls

Cat. No. Product Name / Activity
6969 cis VH 032, amine dihydrochloride
Negative control for VH 032, amine (Cat. No. 6462)
7716 N-methylated pomalidomide
Functionalized cereblon ligand for generating Degrader negative controls; also used as Pomalidomide negative control

Literature for Functionalized E3 Ligase Ligands

Tocris offers the following scientific literature for Functionalized E3 Ligase Ligands 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 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