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Ubiquitin Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	E1/E2/E3 Enzyme (30) ADC Cytotoxin (1) Akt (2) Antibiotic (1) Apoptosis (22) Aryl Hydrocarbon Receptor (1) Autophagy (4) Bacterial (2) Bcl-2 Family (3) BCL6 (1) Btk (1) c-Met/HGFR (1) Caspase (2) Deubiquitinase (34) DNA/RNA Synthesis (1) E3 Ligase Ligand-Linker Conjugates (4) EGFR (3) Endogenous Metabolite (1) Epigenetic Reader Domain (2) ERK (1) Estrogen Receptor/ERR (1) HDAC (1) Hexokinase (1) HIF/HIF Prolyl-Hydroxylase (1) Histone Methyltransferase (1) IKK (2) Isotope-Labeled Compounds (1) Ligands for E3 Ligase (8) Ligands for Target Protein for PROTAC (2) MDM-2/p53 (10) Microtubule/Tubulin (1) Molecular Glues (4) MyD88 (1) NAMPT (1) NF-κB (3) p97 (2) Parasite (2) PROTACs (14) Proteasome (6) Proton Pump (1) Raf (1) Sirtuin (1) SNIPERs (4) STAT (1) Topoisomerase (1)
By Research Areas:	Cancer (104) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (14) Metabolic Disease (1) Neurological Disease (3)
Click Chemistry:	Azide (3)

120

Inhibitors & Agonists

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Peptides

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Products

Isotope-Labeled Compounds

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Targets Recommended: E1/E2/E3 Enzyme

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-150505

DC-U4106	Deubiquitinase Apoptosis	Cancer
DC-U4106 is a USP8 targeting inhibitor with the K_dvalue of 4.7 μM and the IC₅₀ value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer .

HY-W054146

RAMB4 1 Publications Verification	Proteasome	Cancer
RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity .

HY-47879

WAY-304671

Others Others

WAY-304671 is an active molecule and a potential ubiquitin ligase inhibitor.

WAY-304671	Others	Others
WAY-304671 is an active molecule and a potential ubiquitin ligase inhibitor.

HY-W145436

Thalidomide-Piperazine 5-fluoride hydrochloride	Ligands for E3 Ligase	Cancer
Thalidomide-Piperazine 5-fluoride hydrochloride is a derivative of cereblon (CRBN) inhibitor Thalidomide (HY-14658), which can be used as ligands for E3 ubiquitin ligase (Ligands for E3 Ligase) for PROTACs Synthesis .

HY-103436

NSC624206	E1/E2/E3 Enzyme	Cancer
NSC624206 is an inhibitor of ubiquitin E1 (UBA1), with an IC₅₀ of ~9 μM. NSC624206 specifically blocks ubiquitin-thioester formation (IC₅₀=13 μM) but has no effect on ubiquitin adenylation .

HY-120204

BI8626

1 Publications Verification

E1/E2/E3 Enzyme Cancer

BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC₅₀ of 0.9 μM .
HY-120929

BI8622

3 Publications Verification

E1/E2/E3 Enzyme Cancer

BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC₅₀ of 3.1 μM .
HY-17540

HBX 19818

10+ Cited Publications

Deubiquitinase Cancer

HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC₅₀ of 28.1 μM.

BI8626 1 Publications Verification	E1/E2/E3 Enzyme	Cancer
BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC₅₀ of 0.9 μM .

BI8622 3 Publications Verification	E1/E2/E3 Enzyme	Cancer
BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC₅₀ of 3.1 μM .

HBX 19818 10+ Cited Publications	Deubiquitinase	Cancer
HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC₅₀ of 28.1 μM.

HY-143715

Cereblon inhibitor 1	Ligands for E3 Ligase	Cancer
Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating agent. Cereblon inhibitor 1 has the potential for cancer research.

HY-50736

DUB-IN-1

5 Publications Verification

Deubiquitinase Cancer

DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC₅₀ of 0.85 μM for USP8 .

DUB-IN-1 5 Publications Verification	Deubiquitinase	Cancer
DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC₅₀ of 0.85 μM for USP8 .

HY-100739

RA190 3 Publications Verification	Proteasome	Cancer
RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

HY-18327

HLI98C

E1/E2/E3 Enzyme MDM-2/p53 Cancer

HLI98C is a ubiquitin ligase inhibitor. HLI98C inhibits p53 ubiquitylation. HLI98C inhibits HDM2 auto-ubiquitylation .

HLI98C	E1/E2/E3 Enzyme MDM-2/p53	Cancer
HLI98C is a ubiquitin ligase inhibitor. HLI98C inhibits p53 ubiquitylation. HLI98C inhibits HDM2 auto-ubiquitylation .

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-112128

USP7-IN-3

Deubiquitinase Cancer

USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor .
HY-138698

FT206

Deubiquitinase Others

FT206 is an inhibitor of carboxamides as ubiquitin-specific protrase extracted from patent WO 2020033707 A1, example 11-1 .
HY-148481

USP7-IN-10

Deubiquitinase Cancer

USP7-IN-10 (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC₅₀ of 13.39 nM .
HY-148481A

USP7-IN-10 hydrochloride

Deubiquitinase Cancer

USP7-IN-10 hydrochloride (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC₅₀ of 13.39 nM .
HY-15667

P005091

10+ Cited Publications

P5091
Deubiquitinase Cancer

P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC₅₀ of 4.2 μM.

USP7-IN-3	Deubiquitinase	Cancer
USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor .

FT206	Deubiquitinase	Others
FT206 is an inhibitor of *carboxamides as ubiquitin-specific protrase* extracted from patent WO 2020033707 A1, example 11-1 .

USP7-IN-10	Deubiquitinase	Cancer
USP7-IN-10 (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC₅₀ of 13.39 nM .

USP7-IN-10 hydrochloride	Deubiquitinase	Cancer
USP7-IN-10 hydrochloride (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC₅₀ of 13.39 nM .

P005091 10+ Cited Publications P5091	Deubiquitinase	Cancer
P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC₅₀ of 4.2 μM.

HY-12990

Spautin-1 5+ Cited Publications	Autophagy Apoptosis Deubiquitinase	Cancer
Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC₅₀s of 0.6-0.7 μM.

HY-134417

NSC2805	Others	Cancer
NSC2805 is a *WWP2 ubiquitin* ligase** inhibitor that can significant inhibit WWP2 activity with an IC₅₀ of 0.38 μM. NSC2805 can be used for the research of cancer .

HY-100487

TAK-243 25+ Cited Publications 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-13296

PYR-41 10+ Cited Publications	E1/E2/E3 Enzyme Apoptosis	Cancer
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC₅₀ of < 10 μM, with little activity at E2 and E3.

HY-16709

USP7-IN-1 4 Publications Verification	Deubiquitinase	Cancer
USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC₅₀ of 77 μM, and can be used for the research of cancer.

HY-13865

P 22077 10+ Cited Publications	Deubiquitinase	Cancer
P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC₅₀ of 8.01 μM. P 22077 also inhibits USP47 with an EC₅₀ of 8.74 μM.

HY-12989

LDN-91946	Deubiquitinase	Neurological Disease Cancer
LDN-91946 is a potent, selective and uncompetitive ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitor with a K_{i app} of 2.8 μM .

HY-148099

USP1-IN-2

Deubiquitinase Cancer

USP1-IN-2 (Compound I-193) is a potent ubiquitin-specific protease 1 (USP1) inhibitor with an IC₅₀ of less than about 50 nM .

USP1-IN-2	Deubiquitinase	Cancer
USP1-IN-2 (Compound I-193) is a potent ubiquitin-specific protease 1 (USP1) inhibitor with an IC₅₀ of less than about 50 nM .

HY-114304

COH000 1 Publications Verification	E1/E2/E3 Enzyme	Cancer
COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC₅₀ of 0.2 μM for SUMOylation in vitro .

HY-15301

CC0651	E1/E2/E3 Enzyme	Cancer
CC0651 is an allosteric inhibitor of the human *Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC₅₀=1.72 μM) inhibits* the ubiquitination of p27 ^Kip1, as confirmed by dose-response analysis.

HY-N0170

Indole-3-carbinol 5+ Cited Publications I3C; 3-Indolemethanol	NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Endogenous Metabolite	Cancer
Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).

HY-W598456

Brigimadlin intermediate-1	Others	Cancer
Brigimadlin intermediate-1 is an intermediate of the E3 ubiquitin protein ligase MDM-2 inhibitor Brigimadlin (HY-152859) and can be used to synthesize Antibody-Drug Conjugates (ADCs) .

HY-16658B

Z-VAD-FMK Maximum Cited Publications 297 Publications Verification Z-VAD(OH)-FMK	Caspase Apoptosis	Cancer
Z-VAD-FMK (Z-VAD(OH)-FMK) is a well-know pan caspase inhibitor, which does not inhibit ubiquitin carboxy-terminal hydrolase L1 (UCHL1) activity even at concentrations as high as 440 μM .

HY-108640A

HLI373 dihydrochloride	MDM-2/p53 Parasite Apoptosis	Infection Cancer
HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents . Antimalarial activity .

HY-108640

HLI373	MDM-2/p53 Parasite Apoptosis	Infection Cancer
HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents . Antimalarial activity .

HY-129169

USP7-IN-6

Deubiquitinase Cancer

USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC₅₀ of 6.8 nM .

USP7-IN-6	Deubiquitinase	Cancer
USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC₅₀ of 6.8 nM .

HY-N10332

Leptosphaerodione	Proteasome	Cancer
Leptosphaerodione, isolated from Remotididymella sp. Fungus, is a potent ubiquitin-proteasome system (UPS) inhibitor. Leptosphaerodione exhibits cytotoxicity in HeLa cells with IC₅₀ value of 3.2 μM. Anti-tumor agent .

HY-157435

PELI1-IN-1

E1/E2/E3 Enzyme Cancer

PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumor effect .

PELI1-IN-1	E1/E2/E3 Enzyme	Cancer
PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, *E3 ubiquitin* ligase**. PELI1-IN-1 has anti-tumor effect .

HY-135844

LS-102 2 Publications Verification	E1/E2/E3 Enzyme	Inflammation/Immunology
LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC₅₀ of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment .

HY-111879

Biotin-BS	SNIPERs	Cancer
Biotin-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and biotin, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase .

HY-153045

BAY-805	Deubiquitinase	Cancer
BAY-805 is a selective inhibitor of ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common target enzymes .

HY-N2306

Aclacinomycin A 3 Publications Verification Aclarubicin
Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .

HY-N2306A

Aclacinomycin A hydrochloride Aclarubicin hydrochloride	Topoisomerase DNA/RNA Synthesis Proteasome Antibiotic	Cancer
Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .

HY-13487

USP7/USP47 inhibitor 3 Publications Verification	Deubiquitinase	Cancer
USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC₅₀s of 0.42 μM and 1.0 μM, respectively.

HY-110204

Heclin 1 Publications Verification	E1/E2/E3 Enzyme Akt MyD88	Others
Heclin is a *HECT E3 ubiquitin* ligases** inhibitor. Heclin inhibits Smurf2, Nedd4, WWP1 (IC₅₀ values are 6.8, 6.3, 6.9 μM) and can be used for the research of gastric cancer .

HY-111878

BzNH-BS	SNIPERs	Cancer
BzNH-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase .

HY-W062696

BC-1382	E1/E2/E3 Enzyme	Inflammation/Immunology
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC₅₀≈ 5 nM).Anti-inflammatory activity .

HY-12025

Serdemetan 2 Publications Verification JNJ-26854165	MDM-2/p53 E1/E2/E3 Enzyme Apoptosis	Cancer
Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.

HY-130604

DT2216 1 Publications Verification	Bcl-2 Family PROTACs Apoptosis	Cancer
DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax (HY-10087), a linker, and a VHL E3 ubiquitin ligase (Red: Navitoclax; Blue: VHL ligand; Black: linker) .

HY-111623

USP30 inhibitor 11	Deubiquitinase	Cancer
USP30 inhibitor 11 is a selective and potent ubiquitin specific peptidase 30 (USP30) inhibitor with an IC₅₀ of 0.01 µΜ, the example 83 extracted from patent WO2017009650A1. USP30 inhibitor 11 is used for the study of cancer and conditions involving mitochondrial dysfunction .

HY-A0003

Lenalidomide 30+ Cited Publications CC-5013	Ligands for E3 Ligase Molecular Glues Apoptosis	Inflammation/Immunology Cancer
Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a *ligand of ubiquitin* E3 ligase cereblon (CRBN)*, and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin* ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .

HY-A0003B

Lenalidomide hemihydrate 30+ Cited Publications CC-5013 hemihydrate	Ligands for E3 Ligase Molecular Glues Apoptosis	Cancer
Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a *ligand of ubiquitin* E3 ligase cereblon (CRBN)*, and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin* ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0170

Indole-3-carbinol 5+ Cited Publications I3C; 3-Indolemethanol	Alkaloids other families Classification of Application Fields Source classification Plants Endogenous metabolite Disease Research Fields Indole Alkaloids Cancer	NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Endogenous Metabolite
Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).

HY-N7695

Physalin B	other families Classification of Application Fields Ketones, Aldehydes, Acids Source classification Plants Disease Research Fields Cancer	Apoptosis Autophagy
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .

HY-N10332

Leptosphaerodione	Quinones Monophenols Microorganisms Classification of Application Fields Source classification Phenols Naphthalene Quinones Disease Research Fields Cancer	Proteasome
Leptosphaerodione, isolated from Remotididymella sp. Fungus, is a potent ubiquitin-proteasome system (UPS) inhibitor. Leptosphaerodione exhibits cytotoxicity in HeLa cells with IC₅₀ value of 3.2 μM. Anti-tumor agent .

HY-N2306A

Aclacinomycin A hydrochloride Aclarubicin hydrochloride	Quinones Structural Classification Microorganisms Classification of Application Fields Anthraquinones Source classification Phenols Polyphenols Disease Research Fields Cancer	Topoisomerase DNA/RNA Synthesis Proteasome Antibiotic
Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .

Cat. No.	Product Name	Chemical Structure

HY-A0003S

Lenalidomide-d5

Lenalidomide-d₅ is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].

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