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Ubiquitination protein

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) Bcr-Abl (2) CaMK (1) Deubiquitinase (3) DNA/RNA Synthesis (1) E1/E2/E3 Enzyme (3) Endogenous Metabolite (1) HIF/HIF Prolyl-Hydroxylase (1) Histone Methyltransferase (1) Itk (1) Ligands for E3 Ligase (8) Mitophagy (1) NF-κB (1) PROTACs (5) Tau Protein (1) TGF-beta/Smad (1)
By Research Areas:	Cancer (17) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (5)

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Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-124713

ML372	DNA/RNA Synthesis	Neurological Disease
ML372 inhibits survival motor neuron (SMN) protein ubiquitination, increases SMN protein stability without affecting mRNA expression. ML372 improves spinal muscular atrophy (SMA) in mice. ML372 is brain penetrant and has a reasonable exposure and half-life in vivo .

HY-135199

Ubiquitination-IN-1	E1/E2/E3 Enzyme	Cancer
Ubiquitination-IN-1 (compound 24) is a *ubiquitination* and Cksl-Skp2 protein-protein interaction (IC₅₀=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 has the potential for treatment disease by blocking the degradation of tumor suppressors .

HY-156959

Ovalicin	Others	Others
Ovalicin is a potent angiogenesis inhibitor. Ovalicin can be used for the preparation of targeting ubiquitination composition libraries which can be used to identify proteins involved in a predetermined function of cells .

HY-152266

Ubiquitination-IN-2	E1/E2/E3 Enzyme	Cancer
Ubiquitination-IN-2 is a potent *E1-E2 protein−protein* interactions (PPI)** inhibitor. Ubiquitination-IN-2 has a K_d value of 0.72 μM for ubiquitin E1 (Uba1). Ubiquitination-IN-2 inhibits blocks ubiquitin transfer from E1 to E2. Ubiquitination-IN-2 can be used in research of cancer .

HY-153322

ITK degrader 2

Itk Cancer

ITK degrader 2 (compound 30) is a modulator of targeted ubiquitination and a targeted protein degrading molecule. ITK degrader 2 degrades ITK .

ITK degrader 2	Itk	Cancer
ITK degrader 2 (compound 30) is a modulator of targeted ubiquitination and a targeted protein degrading molecule. ITK degrader 2 degrades ITK .

HY-112438

MF-094 3 Publications Verification	Deubiquitinase	Cancer
MF-094 is a potent and selective USP30 inhibitor with an IC₅₀ of 120 nM. MF-094 increases protein ubiquitination and accelerates mitophagy .

HY-141659

CMPD-39 1 Publications Verification	Deubiquitinase	Cancer
CMPD-39 is a selective USP30 inhibitor with an IC₅₀ of 0.02 μM. CMPD-39 increases protein ubiquitination and accelerates mitophagy .

HY-128807

E3 ligase Ligand 10	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .

HY-129653

E3 ligase Ligand 18	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .

HY-128811

E3 ligase Ligand 14	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .

HY-43961

E3 ligase Ligand 8 3 Publications Verification	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .

HY-128810

E3 ligase Ligand 13	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .

HY-128806

E3 ligase Ligand 9	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .

HY-W020033

Lanosterol 2 Publications Verification	Endogenous Metabolite	Neurological Disease
Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol suppresses the aggregation and cytotoxicity of misfolded proteins linked with neurodegenerative diseases .

HY-138669

C004019	PROTACs Tau Protein	Neurological Disease
C004019 is a small-molecule PROTAC. C004019 simultaneously recruites tau and E3-ligase (Vhl) and thus selectively enhances ubiquitination and proteolysis of tau proteins. C004019 can be used for Alzheimer disease (AD) research .

HY-147373

DA-PROTAC	PROTACs Ligands for E3 Ligase	Cancer
DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research .

HY-125834

GMB-475	PROTACs Bcr-Abl Apoptosis	Cancer
GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent agent resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein .

HY-130297

PROTAC BCR-ABL1 ligand 1	Bcr-Abl	Cancer
PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1 .

HY-157428

USP3 ZnF-UBD ligand-1

Others Others

USP3 ZnF-UBD ligand-1 (compound 59) is a ligand that binds to the zinc finger ubiquitin-binding domain (ZnF-UBD) of USP3 with a K_D of 14 μM .

USP3 ZnF-UBD ligand-1	Others	Others
USP3 ZnF-UBD ligand-1 (compound 59) is a ligand that binds to the zinc finger ubiquitin-binding domain (ZnF-UBD) of USP3 with a K_D of 14 μM .

HY-157416

COP1-ATGL modulator 1	Others	Metabolic Disease
COP1-ATGL modulator 1 (86) is an orally active modulator for COP1-ATGL axis. COP1-ATGL modulator 1 (86) could increase ATGL protein expression, reduce ATGL ubiquitination and COP1 autoubiquitination, and diminish lipid accumulation in hepatocytes in the nanomolar range .

HY-160019

MTX115325	Deubiquitinase Mitophagy	Neurological Disease
MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC₅₀=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC₅₀=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .

HY-100487

TAK-243 Maximum Cited Publications 29 Publications Verification MLN7243	E1/E2/E3 Enzyme NF-κB Apoptosis	Cancer
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC₅₀=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis .

HY-130269

β-Naphthoflavone-CH2-OH β-NF-CH2-OH	Ligands for E3 Ligase	Cancer
β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .

HY-147025

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine 1 Publications Verification	PROTACs TGF-beta/Smad HIF/HIF Prolyl-Hydroxylase	Inflammation/Immunology
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine has a multi-path anti-fibrosis function and a renal protection function for research of renal anemia .

HY-156104

CaMKIIα-PHOTAC	PROTACs CaMK	Neurological Disease
CaMKIIα-PHOTAC is a photochemically targeted chimera (PHOTAC) targeting Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα). Molecules such as PHOTAC can catalyze the ubiquitination and degradation of target proteins through the endogenous proteasome under specific wavelengths of light. CaMKIIα-PHOTAC reduces synaptic function under light conditions, and it attenuates the intensity of evoked field excitatory postsynaptic potentials in the mouse hippocampus in response to physiological stimuli. CaMKIIα-PHOTAC plays a critical role in maintaining long-term potentiation and memory capacity in subcellular dendritic domains .

HY-101508

GNA002	Histone Methyltransferase	Cancer
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC₅₀ of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .

Cat. No.	Product Name

HY-L050

Ubiquitination Compound Library	257 compounds
Protein ubiquitination is an enzymatic post-translational modification in which an ubiquitin protein is attached to a substrate protein. Ubiquitination involves three main steps: activation, conjugation, and ligation, performed by ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s), and ubiquitin ligases (E3s), respectively. Ubiquitination affects cellular processes such as apoptosis, cell cycle, DNA damage repair, and membrane transportation, etc. by regulating the degradation of proteins (via the proteasome and lysosome), altering the cellular localization of proteins, affecting proteins activity, and promoting or preventing protein-protein interactions. Deregulation of ubiquitin pathway leads to many diseases such as neurodegeneration, cancer, infection and immunity, etc. MCE offers a unique collection of 257 small molecule modulators with biological activity used for ubiquitination research. Compounds in this library target the key enzymes in ubiquitin pathway. MCE Ubiquitination Compound Library is a useful tool for the research of ubiquitination regulation and the corresponding diseases.

Ubiquitination Compound Library

257 compounds

Protein ubiquitination is an enzymatic post-translational modification in which an ubiquitin protein is attached to a substrate protein. Ubiquitination involves three main steps: activation, conjugation, and ligation, performed by ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s), and ubiquitin ligases (E3s), respectively. Ubiquitination affects cellular processes such as apoptosis, cell cycle, DNA damage repair, and membrane transportation, etc. by regulating the degradation of proteins (via the proteasome and lysosome), altering the cellular localization of proteins, affecting proteins activity, and promoting or preventing protein-protein interactions. Deregulation of ubiquitin pathway leads to many diseases such as neurodegeneration, cancer, infection and immunity, etc.

MCE offers a unique collection of 257 small molecule modulators with biological activity used for ubiquitination research. Compounds in this library target the key enzymes in ubiquitin pathway. MCE Ubiquitination Compound Library is a useful tool for the research of ubiquitination regulation and the corresponding diseases.

HY-L137

Molecular Glue Compound Library	39 compounds
Targeted protein degradation(TPD) is a novel and promising approach to new drug discovery and development. It shows great potential for treating diseases with “undruggable” pathogenic protein targets and for overcoming drug resistance. Molecular glues and PROTACs are both targeted protein degraders that have attracted the most attention. Molecular glues are small molecular degraders that mainly induce novel interaction between an E3 ligase and a target protein to form a ternary complex, leading to protein ubiquitination and subsequent proteasome degradation. Compared with PROTACs, molecular glues generally possess more favorable drug-like properties, such as lower MW, higher cell permeability, and better oral absorption. Molecular glues are emerging as a promising new therapeutic strategy. MCE supplies a unique collection of 39 molecular glues which target various proteins. MCE Molecular Glue Compound Library is a useful tool to conduct scientific research and disease mechanism study.

Molecular Glue Compound Library

39 compounds

Targeted protein degradation(TPD) is a novel and promising approach to new drug discovery and development. It shows great potential for treating diseases with “undruggable” pathogenic protein targets and for overcoming drug resistance. Molecular glues and PROTACs are both targeted protein degraders that have attracted the most attention.

Molecular glues are small molecular degraders that mainly induce novel interaction between an E3 ligase and a target protein to form a ternary complex, leading to protein ubiquitination and subsequent proteasome degradation. Compared with PROTACs, molecular glues generally possess more favorable drug-like properties, such as lower MW, higher cell permeability, and better oral absorption. Molecular glues are emerging as a promising new therapeutic strategy.

MCE supplies a unique collection of 39 molecular glues which target various proteins. MCE Molecular Glue Compound Library is a useful tool to conduct scientific research and disease mechanism study.

HY-L129

Target Protein Ligand Library	39 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. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance. MCE carefully prepared a unique collection of 39 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

Target Protein Ligand Library

39 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. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

MCE carefully prepared a unique collection of 39 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

HY-L128

E3 Ligase Ligand Library	58 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 58 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

58 compounds

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 58 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.

Lanosterol 2 Publications Verification	Triterpenes Structural Classification Human Gut Microbiota Metabolites Microorganisms Terpenoids Source classification Endogenous metabolite	Endogenous Metabolite
Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol suppresses the aggregation and cytotoxicity of misfolded proteins linked with neurodegenerative diseases .

Species:	Human (3)
Tag:	His (1) Tag Free (1) GST (1)
Source:	E. coli (3)

Cat. No.	Compare	Product Name	Species	Source

HY-P701512

	SMURF2 Protein, Human (His) SMURF2; E3 ubiquitin-protein ligase SMURF2; hSMURF2; HECT-type E3 ubiquitin transferase SMURF2; SMAD Ubiquitination regulatory factor 2; SMAD-specific E3 ubiquitin-protein ligase 2	Human	E. coli
	SMURF2 protein is an E3 ubiquitin protein ligase that interacts with SMAD7 to induce ubiquitin-dependent degradation of TGF-β receptors and downregulate TGF-β signaling. This interaction triggers autocatalytic degradation of SMURF2 and is antagonized by AIMP1. SMURF2 Protein, Human (His) is the recombinant human-derived SMURF2 protein, expressed by E. coli , with N-6*His labeled tag. The total length of SMURF2 Protein, Human (His) is 747 a.a., .

HY-P701513

	SMURF2 Protein, Human SMURF2; E3 ubiquitin-protein ligase SMURF2; hSMURF2; HECT-type E3 ubiquitin transferase SMURF2; SMAD Ubiquitination regulatory factor 2; SMAD-specific E3 ubiquitin-protein ligase 2	Human	E. coli
	SMURF2 protein is an E3 ubiquitin protein ligase that interacts with SMAD7 to induce ubiquitin-dependent degradation of TGF-β receptors and downregulate TGF-β signaling. This interaction triggers autocatalytic degradation of SMURF2 and is antagonized by AIMP1. SMURF2 Protein, Human is the recombinant human-derived SMURF2 protein, expressed by E. coli , with tag free. The total length of SMURF2 Protein, Human is 747 a.a., .

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
	UBAC1 protein, a non-catalytic component of the KPC complex, aids in polyubiquitination, targeting proteins like CDKN1B and NFKB1. The KPC complex regulates the cell cycle by ubiquitinating and degrading CDKN1B during the G1 phase. Additionally, it influences NF-kappa-B signaling by promoting NFKB1 maturation. Within the KPC complex, UBAC1 acts as an adapter, facilitating the transfer of polyubiquitinated proteins to the proteasome, emphasizing its role in protein ubiquitination processes. 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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