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E3 ubiquitin ligase complex

" in MedChemExpress (MCE) Product Catalog:

By Targets:	E1/E2/E3 Enzyme (2) Ligands for E3 Ligase (3) Apoptosis (3) Autophagy (3) Btk (1) Molecular Glues (4) NF-κB (1) PROTACs (1)
By Research Areas:	Cancer (6) Inflammation/Immunology (3)

Inhibitors & Agonists

Screening Libraries

Recombinant Proteins

Isotope-Labeled Compounds

Targets Recommended: Ligands for E3 Ligase E3 Ligase Ligand-Linker Conjugates E1/E2/E3 Enzyme SWI/SNF Complex Arp2/3 Complex

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153357

NRX-0492	PROTACs Btk	Cancer
NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC₅₀ ≤ 0.2 nM, DC₉₀ ≤ 0.5 nM) . NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 can bind non-covalently to the BTK binding domain and cereblon, which is an adapter protein in the E3 ubiquitin ligase complex . NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263). E3 ubiquitin ligase and linker can form Thalidomide 5-pyrrolidine-CHO (HY-49372A); the active control for the target protein ligand is BTK ligand 12 (HY-49421).

HY-14658

Thalidomide 15+ Cited Publications	Ligands for E3 Ligase Autophagy Apoptosis Molecular Glues	Inflammation/Immunology Cancer
Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a K_d of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.

HY-49444

EN450	NF-κB Molecular Glues E1/E2/E3 Enzyme	Cancer
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the *E2 ubiquitin* ligase UBE2D*. EN450 induces the ternary complex* formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .

HY-14658R

Thalidomide (Standard)	Ligands for E3 Ligase Autophagy Apoptosis	Inflammation/Immunology Cancer
Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a K_d of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.

HY-170430

HGC652	Molecular Glues E1/E2/E3 Enzyme	Cancer
HGC652 is the molecular glue, that targets E3 ubiquitin ligase TRIM21, promotes the formation of a ternary complex between TRIM21 and NUP98, induces degradation of NUP155 and nuclear pore complex proteins, thereby causing the cell death. HGC652 inhibits the proliferation of multi cancer cells, according to the expression level of TRIM21 .

HY-14658S

Thalidomide-d4	Molecular Glues Ligands for E3 Ligase Autophagy Apoptosis	Inflammation/Immunology Cancer
Thalidomide-d₄ is a deuterium labeled Thalidomide. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties[1][2].

Cat. No.	Product Name

HY-L128

E3 Ligase Ligand Library	65 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 65 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

65 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 65 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.

Cat. No.	Compare	Product Name	Species	Source

HY-P700392

	UBAC1 Protein, Human (GST) UBAC1; UBA domain containing 1; UBADC1, ubiquitin associated domain containing 1; ubiquitin-associated domain-containing protein 1; GBDR1; UBA domain-containing protein 1; E3 ubiquitin-protein ligase subunit KPC2; ubiquitin associated domain containing 1; kip1 ubiquitination-promoting complex protein 2; glialblastoma cell differentiation-related protein 1; putative glialblastoma cell differentiation-related protein; UBADC1; RP11-432J22.3	Human	E. coli
	The UBAC1 protein is a non-catalytic component of the KPC complex and contributes to polyubiquitination, targeting proteins such as CDKN1B and NFKB1. The KPC complex regulates the cell cycle by ubiquitinating and degrading CDKN1B during G1 phase. UBAC1 Protein, Human (GST) is the recombinant human-derived UBAC1 protein, expressed by E. coli , with N-GST labeled tag. The total length of UBAC1 Protein, Human (GST) is 405 a.a., with molecular weight of 72.3 kDa.

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Thalidomide-d4
Thalidomide-d₄ is a deuterium labeled Thalidomide. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties[1][2].

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