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Ligands for E3 Ligase

A PROTAC (Proteolysis Targeting Chimeric Molecule) is a protein degrader comprised of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand for target protein (target binder).The transfer of ubiquitin and degradation of the targeted protein will occur as a result of the connection between an E3 ligase and a target protein brought on by a PROTAC.

E3 ligases determine the specificity of the proteins by catalyzing the transfer of ubiquitin to the desired proteins. Cells have hundreds of E3 ligases, but only a small number of them have been successfully exploited in PROTACs, including VHL (the tumor suppressor protein for von Hippel-Lindau disease), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue), and IAP (inhibitor of apoptosis).

Ligands for E3 Ligase related products

Structure Cat No. Product Name CAS No. Product Description
3-Azathalidomide V125299 3-Azathalidomide 31804-66-7 3-Azathalidomide is a thalidomide analogue that can be used in PROTAC studies.
4-[(1E)-2-Nitroethenyl]benzoic acid V126098 4-[(1E)-2-Nitroethenyl]benzoic acid 821797-33-5 4-[(1E)-2-Nitroethenyl]benzoic acid is an E3 ligand.
4-Boc-amino-2,2-dimethylbutyric acid V82543 4-Boc-amino-2,2-dimethylbutyric acid 153039-17-9 4-Boc-amino-22-dimethylbutyric acid is a PROTAC (PROteolysis TArgeting Chimera) linker of the alkyl/ether class, may be utilized to prepare PROTAC protein degraders.
4-Br-7-O-Desamino lenalidomide V113098 4-Br-7-O-Desamino lenalidomide 2438241-00-8 4-Bromo-7-O-deaminolenalidomide is the E3 ubiquitin ligand of cereblon (CRBN) and is used to recruit cereblon protein.
4-Chloro-3-(2,4-dioxo-1,3-diazinan-1-yl)benzoic acid V126318 4-Chloro-3-(2,4-dioxo-1,3-diazinan-1-yl)benzoic acid 2377645-90-2 4-Chloro-3-(2,4-dioxo-1,3-diazinan-1-yl)benzoic acid is an E3 ligase ligand that can be used to recruit CRBN protein.
4-Me-Thalidomide V126430 4-Me-Thalidomide 244057-31-6 4-Me-Thalidomide is a methyl-containing E3 ubiquitin ligase activator.
4-Methylanisole-dihydrouracil-imidazo[1,2-a]pyridine-piperidine-NH-Boc V83736 4-Methylanisole-dihydrouracil-imidazo[1,2-a]pyridine-piperidine-NH-Boc
5,6-Difluoro-desamino lenalidomide V113492 5,6-Difluoro-desamino lenalidomide 2438241-40-6 5,6-Difluorodeaminyllenalidomide is the E3 ubiquitin ligand for cereblon (CRBN) and is used to recruit cereblon proteins.
5-(2-Chloroacetamide) thalidomide V126558 5-(2-Chloroacetamide) thalidomide 1957235-51-6 5-(2-Chloroacetamide) thalidomide is an analogue of thalidomide.
5-(Biotinamido)pentylazide V82524 5-(Biotinamido)pentylazide 1349190-76-6 5-Biotinamidopentylazide is a PROTAC (PROteolysis TArgeting Chimera) linker and belongs to the alkyl chain class, may be utilized to prepare PROTAC molecules.
5-Br-6-F-Desamino lenalidomide V112787 5-Br-6-F-Desamino lenalidomide 2409005-96-3 5-Br-6-F-deaminolenalidomide is the E3 ubiquitin ligand for cereblon (CRBN) and is used to recruit cereblon proteins.
5-Bromomethylthalidomide V126918 5-Bromomethylthalidomide 1312023-72-5 5-Bromomethylthalidomide is an E3 ligase activator that can be further derivatized by bromide substitution.
5-Fluoro-lenalidomide V113400 5-Fluoro-lenalidomide 1918158-58-3 5-Fluorenalidomide is the E3 ubiquitin ligand of cereblon (CRBN) and can recruit cereblon proteins.
5-Fluoro-pomalidomide V112761 5-Fluoro-pomalidomide 2713422-01-4 5-Fluoropomalidamine is the E3 ubiquitin ligand of cereblon (CRBN) and can recruit cereblon proteins.
5-Hydrazinyl thalidomide hydrochloride V127023 5-Hydrazinyl thalidomide hydrochloride 2803460-96-8 5-Hydrazinyl thalidomide hydrochloride is a thalidomide analog containing a hydrazine group.
5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione V127030 5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione 2589697-74-3 5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione is a thalidomide analogue containing a hydroxyl group in its structure, which is an ideal site for further derivatization.
5-Norbornene-2-methylamine V127134 5-Norbornene-2-methylamine 95-10-3 5-Norbornene-2-methylamine is a hydrophobic label.
6-(2,4-Dioxopyrimidin-1-yl)-1-methylindole V119790 6-(2,4-Dioxopyrimidin-1-yl)-1-methylindole 2766178-76-9 6-(2,4-dioxanil-1-yl)-1-methylindole is an E3 ligase ligand that can be used to synthesize PROTAC androgen receptor degrader-1.
7-F-4-I-Desamino lenalidomide V113443 7-F-4-I-Desamino lenalidomide 2207569-51-3 7-F-4-I-deaminolenalidomide is the E3 ubiquitin ligand for cereblon (CRBN) and is used to recruit cereblon protein.
A 410099.1 amide-PEG2-amine-Boc V82556 A 410099.1 amide-PEG2-amine-Boc 2415256-16-3 410099.1 amide-PEG2-amine-Boc is a functionalized IAP ligand for PROTAC, which combines an IAP ligand and an amide-PEG2 linker with an amide terminal to bind to the target protein ligand.
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