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E3 ubiquitin ligase binding linker

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Ligands for Target Protein for PROTAC (1) Target Protein Ligand-Linker Conjugates (1) CDK (1) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (2) Histone Acetyltransferase (1) MDM-2/p53 (1) PROTACs (5)
By Research Areas:	Cancer (7)

Inhibitors & Agonists

Screening Libraries

Targets Recommended: E3 Ligase Ligand-Linker Conjugates Ligands for E3 Ligase Penicillin-binding protein (PBP) E1/E2/E3 Enzyme ADC Linker Target Protein Ligand-Linker Conjugates PROTAC-Linker Conjugates for PAC Drug-Linker Conjugates for ADC FKBP FABP Transthyretin (TTR) Ligands for Target Protein for PROTAC YB-1 GHR P-glycoprotein

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-123937

THAL-SNS-032 3 Publications Verification	PROTACs CDK	Cancer
THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a *CDK*-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN) .

HY-112098

PROTAC ERα Degrader-1	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.

HY-153424

PROTAC SMARCA2 degrader-1	Target Protein Ligand-Linker Conjugates	Cancer
PROTAC SMARCA2 degrader-1 (compound ex7) is a BRM2 (SMARCA2) degrader (DC₅₀<0.1 μM). PROTAC SMARCA2 degrader-1 is also an E3 ubiquitin ligase binding linker useful in research of cancers. PROTAC SMARCA2 degrader-1 is a *target protein ligand-linker* conjugate** .

HY-145071

PROTAC ERα Y537S degrader-1	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 extracts from patent WO2021143822, example 12. PROTAC ERα Y537S degrader-1 is an estrogen receptor-alpha (ERα) Y537S degrader .

HY-161960

EP300/CBP ligand 2	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
EP300/CBP ligand 2 (compound S19) is a ligand targeting the bromodomain of CREB binding protein (CBP) and E1A-associated protein (EP300). EP300/CBP ligand 2 can be used as a target protein ligand in the PROTAC structure, and can be coupled to the E3 ubiquitin ligase ligand through the PTOTAC Linker to synthesize PROTAC molecules with degradation effects. For example, EP300/CBP ligand 2 can be coupled with the conjugate (E3 ubiquitin enzyme ligand + Linker) Thalidomide-NH-C10-Boc (HY-161961) to produce the PROTAC molecule dCE-2 (HY-161958) .

HY-161958

dCE-2	PROTACs Histone Acetyltransferase	Cancer
dCE-2 (compound 5) is a PROTAC targeting CREB binding protein (CBP) and E1A-associated protein (EP300), which was developed based on the crystal structure of bromodomain (BRD) inhibitors. dCE-2 is composed of E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), PROTAC Linker tert-Butyl 11-aminoundecanoate (HY-130715) (black part) and PROTAC target protein ligand EP300/CBP ligand 2 (HY-161960) (red part), of which the target protein ligand activity control is EP300/CBP ligand 1 (HY-161959), and the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C10-Boc (HY-161961) ^{[1] ^.}

HY-158684

YX-02-030	PROTACs MDM-2/p53	Cancer
YX-02-030M is a PROTAC MDM2 degrader. YX-02-030M inhibits MDM2-p53 binding and VHL-HIF1α binding with IC₅₀s of 63 nM and 1.35 μM respectively. YX-02-030M binds MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, and effectively kills p53 mutant or deleted Triple-negative breast cancers (TNBC) cells. (Blue: VHL ligand; Black: linker; Pink: MDM2 inhibitor) .

Cat. No.	Product Name

HY-L128

E3 Ligase Ligand Library	55 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2). MCE carefully prepared a unique collection of 55 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

E3 Ligase Ligand Library

55 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation.

Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).

MCE carefully prepared a unique collection of 55 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

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