Search Result

Results for "

Proteasome inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Proteasome (88) Akt (4) Androgen Receptor (2) Antibiotic (1) Apoptosis (48) Autophagy (19) Bacterial (9) Bcl-2 Family (3) BCL6 (1) Bcr-Abl (1) Btk (1) c-Met/HGFR (2) Calcium Channel (1) Caspase (1) ClpP (1) Deubiquitinase (7) DNA/RNA Synthesis (1) Drug-Linker Conjugates for ADC (1) E1/E2/E3 Enzyme (3) E3 Ligase Ligand-Linker Conjugates (1) EGFR (3) Endogenous Metabolite (8) Epigenetic Reader Domain (1) Ferroptosis (6) FLT3 (2) Fungal (4) HDAC (2) Hexokinase (1) Histone Methyltransferase (5) HIV (6) IKK (1) Interleukin Related (1) Isotope-Labeled Compounds (1) JAK (2) Keap1-Nrf2 (2) Lipoxygenase (1) Mitophagy (2) MMP (2) NAMPT (2) NEKs (1) NF-κB (11) NOD-like Receptor (NLR) (1) Oxidative Phosphorylation (1) p97 (1) Parasite (7) PARP (2) PERK (1) Phosphodiesterase (PDE) (1) PROTACs (21) RAD51 (2) Raf (2) RAR/RXR (1) Ras (1) Reactive Oxygen Species (1) Ribosomal S6 Kinase (RSK) (1) ROS Kinase (1) Ser/Thr Protease (1) Sigma Receptor (1) SNIPERs (2) STAT (2) Wnt (3) YAP (1) β-catenin (5)
By Research Areas:	Cancer (124) Cardiovascular Disease (2) Infection (16) Inflammation/Immunology (26) Metabolic Disease (8) Neurological Disease (10)

By Targets:

Proteasome (88)

Akt (4)

Androgen Receptor (2)

Antibiotic (1)

Apoptosis (48)

Autophagy (19)

Bacterial (9)

Bcl-2 Family (3)

BCL6 (1)

Bcr-Abl (1)

Btk (1)

c-Met/HGFR (2)

Calcium Channel (1)

Caspase (1)

ClpP (1)

Deubiquitinase (7)

DNA/RNA Synthesis (1)

Drug-Linker Conjugates for ADC (1)

E1/E2/E3 Enzyme (3)

E3 Ligase Ligand-Linker Conjugates (1)

EGFR (3)

Endogenous Metabolite (8)

Epigenetic Reader Domain (1)

Ferroptosis (6)

FLT3 (2)

Fungal (4)

HDAC (2)

Hexokinase (1)

Histone Methyltransferase (5)

HIV (6)

IKK (1)

Interleukin Related (1)

Isotope-Labeled Compounds (1)

JAK (2)

Keap1-Nrf2 (2)

Lipoxygenase (1)

Mitophagy (2)

MMP (2)

NAMPT (2)

NEKs (1)

NF-κB (11)

NOD-like Receptor (NLR) (1)

Oxidative Phosphorylation (1)

p97 (1)

Parasite (7)

PARP (2)

PERK (1)

Phosphodiesterase (PDE) (1)

PROTACs (21)

RAD51 (2)

Raf (2)

RAR/RXR (1)

Ras (1)

Reactive Oxygen Species (1)

Ribosomal S6 Kinase (RSK) (1)

ROS Kinase (1)

Ser/Thr Protease (1)

Sigma Receptor (1)

SNIPERs (2)

STAT (2)

Wnt (3)

YAP (1)

β-catenin (5)

By Research Areas:

Cancer (124)

Cardiovascular Disease (2)

Infection (16)

Inflammation/Immunology (26)

Metabolic Disease (8)

Neurological Disease (10)

161

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Proteasome

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13259D

MG-132 (negative control)	Others	Cancer
MG-132 negative control is the negative control form of MG-132 (HY-13259). MG-132 is a potent proteasome and calpain inhibitor .

HY-160289

ARI-3144	Proteasome	Cancer
ARI-3144 is an excellent substrate for fibroblast activation protein (FAP). ARI-3144 is a FAP-activated proteasome inhibitor that can be used for the research of solid tumors .

HY-120035

DD1	Proteasome Ribosomal S6 Kinase (RSK) Apoptosis	Cancer
DD1, a *proteasome* inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation .

HY-107412

Proteasome inhibitor IX PS-IX; AM114	Proteasome	Cancer
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC₅₀ value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 ^+/+ cells growth inhibitory activity with an IC₅₀ value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity .

HY-149514

BC-05	Proteasome	Cancer
BC-05 is an orally active and potent inhibitor of CD13 and *proteasome. BC-05 has an IC₅₀* value of 0.13 μM for human CD13 and an IC₅₀ value of 1.39 μM for the 20S proteasome. BC-05 can be used in multiple myeloma research .

HY-144369

Proteasome-IN-4	Proteasome	Cancer
Proteasome-IN-4 is an excellent and non-covalent *proteasome* inhibitor (IC₅₀=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research .

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-158412

BT317	Proteasome Apoptosis	Cancer
BT317 is a blood-brain transmissible mitochondrial Lon peptidase I (LonP1) and CT-L proteasome inhibitor. BT317 can increase the production of reactive oxygen species (ROS) and induce apoptosis in astrocytoma cells. BT317 has antitumor activity .

HY-157032

Proteasome-IN-5	Proteasome	Others
Proteasome-IN-5 (compound 5) is a proteasome inhibitor .

HY-100172

Proteasome-IN-1	Proteasome	Cancer
Proteasome-IN-1 is a *proteasome* inhibitor extracted from patent WO 2013142376 A1.

HY-10227

Bortezomib 145+ Cited Publications PS-341; LDP-341; NSC 681239	Proteasome NF-κB Apoptosis Autophagy	Cancer
Bortezomib (PS-341) is a reversible and selective *proteasome* inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .

HY-108552

MG-115 1 Publications Verification	Proteasome Apoptosis	Cancer
MG-115 is a potent and reversible *proteasome* inhibitor, with K_is of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis .

HY-151195

20S Proteasome-IN-4	Proteasome Parasite	Infection
20S Proteasome-IN-4 (Compound 7) is a brain-penetrant, parasite-selective, orally active 20S proteasome inhibitor with an IC₅₀ of 6.3 nM against T. b. brucei 20S proteasome. 20S Proteasome-IN-4 can be used for the research of human African trypanosomiasis (HAT) .

HY-18741

VR23	Proteasome Apoptosis	Metabolic Disease Cancer
VR23 is a small molecule that potently inhibits the activities of trypsin-like proteasomes (IC₅₀=1 nM), chymotrypsin-like proteasomes (IC₅₀=50-100 nM), and caspase-like proteasomes (IC₅₀=3 μM).

HY-150591

20S Proteasome-IN-3	Proteasome	Cancer
20S Proteasome-IN-3 is a 20S proteasome β5 subunit inhibitor (IC₅₀=1.64 μM) . 20S Proteasome-IN-3 shows anti-tumor proliferation activity .

HY-150590

20S Proteasome-IN-2	Proteasome	Cancer
20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC₅₀ of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M .

HY-10453

Ixazomib 15+ Cited Publications MLN2238	Proteasome Autophagy	Cancer
Ixazomib (MLN2238) is a selective, potent, and reversible *proteasome* inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC₅₀ of 3.4 nM (K_i of 0.93 nM).

HY-156605

Davelizomib	Proteasome	Cancer
Davelizomib is proteasome inhibitor with antineoplastic effect .

HY-135396

(1S,2S)-Bortezomib	Proteasome Apoptosis	Cancer
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective *proteasome* inhibitor, and potently inhibits 20S proteasome (K_i of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans .

HY-10227S

Bortezomib-d8 PS-341-d₈; LDP-341-d₈; NSC 681239-d₈	Proteasome NF-κB Apoptosis Autophagy	Cancer
Bortezomib-d₈ is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].

HY-157212

PARP-1/Proteasome-IN-1	Apoptosis PARP Proteasome	Cancer
PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. *PARP-1/Proteasome*-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombination repair function and induce apoptosis .

HY-10227R

Bortezomib (Standard)	Proteasome NF-κB Apoptosis Autophagy	Cancer
Bortezomib (Standard) is the analytical standard of Bortezomib. This product is intended for research and analytical applications. Bortezomib (PS-341) is a reversible and selective *proteasome* inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .

HY-139331

20S Proteasome-IN-1	Proteasome	Neurological Disease Inflammation/Immunology Cancer
20S Proteasome-IN-1 is a 26S proteasome inhibitor extracted from patent WO2006128196A2 compound 2. 20S Proteasome-IN-1 has the potential for cancer, immune-related disorders, inflammation, ischemic conditions, neurodegenerative disorders and other diseases research .

HY-P1258

PSI Proteasome Inhibitor 1; Z-Ile-Glu(OtBu)-Ala-Leu-CHO	Proteasome	Infection Cancer
PSI (Proteasome Inhibitor 1) is a potent *proteasome* inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas .

HY-119288

BC-23 NSC 45382	Proteasome	Cancer
BC-23 (NSC 45382) is a *proteasome* inhibitor. BC-23 exhibits good inhibition of CT-L activity of the proteasome and is selective for malignant over normal cells .

HY-158150

20S Proteasome-IN-5	Proteasome	Cancer
20S Proteasome-IN-5 (Compound 5) is a macrocyclic inhibitor of the 20S Proteasome, with IC₅₀ values of 0.19 and 52.5 μM for ChT-L and PGPH-L activity, respectively .

HY-P1259

PR-39	Proteasome Bacterial	Inflammation/Immunology
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric *proteasome* inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

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-13067R

Celastrol (Standard)	Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite	Inflammation/Immunology Cancer
Celastrol (Standard) is the analytical standard of Celastrol. This product is intended for research and analytical applications. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM.

HY-P1259A

PR-39 TFA	Proteasome Bacterial	Inflammation/Immunology
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric *proteasome* inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-110404

Capzimin 3 Publications Verification	Proteasome Deubiquitinase	Cancer
Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.

HY-157035

Proteasome β2c/i-IN-1	Proteasome	Others
Proteasome β2c/i-IN-1 (compound 37) is a subunit-selective human proteasome β2c and β2i inhibitor .

HY-168048

ZINC09518833	Proteasome	Cancer
ZINC09518833 is a α-ketoamide nonpeptidic *proteasome* inhibitor with an IC₅₀ value of 12.4 μM. ZINC09518833 binds both primed and nonprimed sites of the proteasome. ZINC09518833 is promising for research of multiple myeloma (MM) .

HY-113824

RID-F Ridaifen-F	Proteasome	Cancer
RID-F (Ridaifen-F), a Tamoxifen (HY-13757A) derivative, is a nonpeptidic *proteasome* inhibitor. RID-F inhibits human 20S proteasome activity, with IC₅₀s of 0.64, 0.34, and 0.43 μM for CT-L, T-L, and PGPH, respectively .

HY-10453R

Ixazomib (Standard)	Proteasome Autophagy	Cancer
Ixazomib (Standard) is the analytical standard of Ixazomib. This product is intended for research and analytical applications. Ixazomib (MLN2238) is a selective, potent, and reversible *proteasome* inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC₅₀ of 3.4 nM (K_i of 0.93 nM).

HY-12471

VLX1570 2 Publications Verification	Deubiquitinase	Cancer
VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC₅₀ of approximate 10 μM.

HY-12113

Oprozomib 1 Publications Verification ONX 0912; PR-047	Proteasome Autophagy Apoptosis	Cancer
Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone *proteasome* inhibitor with IC₅₀s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells .

HY-108551

MG-262 1 Publications Verification	Proteasome	Cardiovascular Disease Inflammation/Immunology Cancer
MG-262 is a reversible proteasome inhibitor with diverse biological activities .

HY-N11620

Sadopeptins A	Proteasome	Others
Sadopeptins A is a nature product that could be isolated from Streptomyces sp. Sadopeptins A is a potent proteasome inhibitor .

HY-164689

Cadmium pyrithione	Others	Cancer
Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models .

HY-10455

Carfilzomib 25+ Cited Publications PR-171	Proteasome Autophagy Apoptosis	Cancer
Carfilzomib (PR-171) is an irreversible *proteasome* inhibitor with an IC₅₀ of 5 nM in ANBL-6 and RPMI 8226 cells.

HY-143535

HG122	Androgen Receptor	Cancer
HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.

HY-N11621

Sadopeptins B	Proteasome	Others
Sadopeptins B is a nature product that could be isolated from Streptomyces sp. Sadopeptins B is a potent proteasome inhibitor .

HY-10985

Marizomib 5+ Cited Publications Salinosporamide A; NPI-0052	Proteasome	Cancer
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, *pan-proteasome* inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively) .

HY-155103

Antitrypanosomal agent 15	Proteasome Parasite	Infection
Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against **Trypanosoma cruzi proteasome, with an _pIC₅₀** of 7.4 and <4 for T. cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study .

HY-13067

Celastrol 30+ Cited Publications Tripterine; Tripterin	Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite Antibiotic Bacterial	Infection Inflammation/Immunology Cancer
Celastrol (Tripterine;Tripterin) is a *proteasome* inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .

HY-127102

GSK3494245 DDD01305143	Parasite Proteasome	Infection
GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite *proteasome* binding in a site sandwiched between the β4 and β5 subunits (IC₅₀=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC₅₀: purified 26S=13 µM; enriched THP-1 extracts IC₅₀=40µM). GSK3494245 exhibits attractive biological and biosafety properties .

HY-169135

PROTAC 20S proteasome subunit β5 degrader 2	PROTACs Proteasome	Cancer
PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader for *20S proteasome* subunit β5, with a DC₅₀** of 0.16 μM. PROTAC 20S proteasome subunit β5 degrader 2 inhibits the proliferation of cancer cell FaDu with IC₅₀ of 0.23 μM. PROTAC 20S proteasome subunit β5 degrader 2 exhibits antitumor efficacy in mice models . (Pink: Ligand for target protein (HY-10227); Blue: Ligand for E3 ligase (HY-103596); Black: Linker (HY-Y1760))

HY-100739

RA190 4 Publications Verification	Proteasome	Cancer
RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

HY-125939

Bortezomib-pinanediol	Proteasome	Cancer
Bortezomib-pinanediol is a *proteasome* inhibitor and a prodrug of Bortezomib (HY-10227). Bortezomib-pinanediol inhibits cell growth and can be used for study of multiple myeloma .

Cat. No.	Product Name

HY-L012

Metabolism/Protease Compound Library

4,645 compounds

Metabolism is the set of life-sustaining chemical reactions in organisms. Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of natural product small molecules within a cell or tissue. Acting as catalysts, enzymes are crucial to metabolism - they allow a reaction to proceed more rapidly - and they also allow the regulation of the rate of a metabolic reaction. Proteases are used throughout an organism for various metabolic processes. Proteases control a great variety of physiological processes that are critical for life, including the immune response, cell cycle, cell death, wound healing, food digestion, and protein and organelle recycling. Imbalances in metabolic activities have been found to be critical in a number of pathologies, such as cardiovascular diseases, inflammation, cancer, and neurodegenerative diseases.

MCE designs a unique collection of 4,645 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.

HY-L050

Ubiquitination Compound Library

258 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 258 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-L129

Target Protein Ligand Library

37 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 37 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

54 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 54 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.	Product Name	Target	Research Area

HY-P1258

PSI Proteasome Inhibitor 1; Z-Ile-Glu(OtBu)-Ala-Leu-CHO	Proteasome	Infection Cancer
PSI (Proteasome Inhibitor 1) is a potent *proteasome* inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas .

HY-P1259A

PR-39 TFA	Proteasome Bacterial	Inflammation/Immunology
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric *proteasome* inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-P5819

xStAx-VHLL	Wnt PROTACs β-catenin	Cancer
xStAx-VHLL is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL can inhibit the proliferation of colon cancer cells and has anti-tumor activity .

HY-P5819A

xStAx-VHLL TFA	PROTACs β-catenin Wnt	Cancer
xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity .

HY-158150

20S Proteasome-IN-5	Proteasome	Cancer
20S Proteasome-IN-5 (Compound 5) is a macrocyclic inhibitor of the 20S Proteasome, with IC₅₀ values of 0.19 and 52.5 μM for ChT-L and PGPH-L activity, respectively .

HY-P1259

PR-39	Proteasome Bacterial	Inflammation/Immunology
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric *proteasome* inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-P4284

Z-GGF-CMK	ClpP Proteasome	Others
Z-GGF-CMK is a protease inhibitor, inhibits ClpP1P2 and proteasome. Z-GGF-CMK exhibits cytotoxic activity against HepG2 cells with a CC₅₀ value of 125 μM .

HY-137281

HMB-Val-Ser-Leu-VE	Ser/Thr Protease	Others
HMB-Val-Ser-Leu-VE is a prototype vinyl ester inhibitor. HMB-Val-Ser-Leu-VE is against trypsin-like (T-L) proteasome activity with an IC₅₀ of 0.033 μM .

HY-P1258A

PSI TFA Proteasome Inhibitor 1 TFA; Z-Ile-Glu(OtBu)-Ala-Leu-CHO TFA	Proteasome	Infection Cancer
PSI (TFA) is a potent *proteasome* inhibitor. PSI (TFA) inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI (TFA) can be used for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas .

HY-P4910

Baceridin	Proteasome Apoptosis	Cancer
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research .

HY-P10438

Tat-braftide	Raf	Cancer
Tat-braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by Tat-braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers .

HY-P10714

Ub4ix	Proteasome Apoptosis Deubiquitinase	Cancer
Ub4ix is a DUB/26S proteasome inhibitor. Ub4ix can protect K48-linked Ub chains from being chopped up by deubiquitinating enzymes (DUBs) and prevent the proteasomal degradation of Ub-tagged proteins. Ub4ix can reduce the viability of Hela cells and induce apoptosis, with an IC₅₀ value of 1.6 μM .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-10985

Marizomib 5+ Cited Publications Salinosporamide A; NPI-0052	Marine natural products Source classification Marine microorganism	Proteasome
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, *pan-proteasome* inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively) .

HY-13067

Celastrol Maximum Cited Publications 35 Publications Verification Tripterine; Tripterin	Triterpenes Structural Classification Classification of Application Fields Anti-aging Terpenoids Source classification Celastraceae Tripterygium wilfordii Hook. f. Plants Inflammation/Immunology Disease Research Fields Cancer	Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite Antibiotic Bacterial
Celastrol (Tripterine;Tripterin) is a *proteasome* inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .

HY-13821

Epoxomicin 10+ Cited Publications BU-4061T	Structural Classification Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Inflammation/Immunology Disease Research Fields	Proteasome Apoptosis
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible *proteasome* inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the *proteasome* and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity .

HY-N2117

Isoginkgetin 10+ Cited Publications	Structural Classification Flavonoids Ginkgoaceae Classification of Application Fields Source classification Phenols Polyphenols Plants Biflavones Ginkgo biloba Disease Research Fields Cancer	MMP Akt NF-κB Proteasome Apoptosis Autophagy
Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy .

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-13067R

Celastrol (Standard)	Triterpenes Structural Classification Terpenoids Source classification Celastraceae Tripterygium wilfordii Hook. f. Plants	Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite
Celastrol (Standard) is the analytical standard of Celastrol. This product is intended for research and analytical applications. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM.

HY-N11620

Sadopeptins A	Structural Classification Monophenols Microorganisms Source classification Phenols	Proteasome
Sadopeptins A is a nature product that could be isolated from Streptomyces sp. Sadopeptins A is a potent proteasome inhibitor .

HY-N11621

Sadopeptins B	Structural Classification Monophenols Microorganisms Source classification Phenols	Proteasome
Sadopeptins B is a nature product that could be isolated from Streptomyces sp. Sadopeptins B is a potent proteasome inhibitor .

HY-108549

clasto-Lactacystin β-lactone Omuralide; β-Clastolactacystin	Classification of Application Fields Disease Research Fields Cancer	Proteasome
Clasto-Lactacystin β-lactone, a natural active metabolite of lactacystin, which is a metabolite of Streptomyces, acts as an irreversible 20S proteasome inhibitor.

HY-N15130

Cerpegin	Apocynaceae Ceropegia junceaRoxb. Structural Classification Alkaloids Source classification Pyridine Alkaloids Plants	Proteasome
Cerpegin, a pyridinone-fused c-lactone, is an inhibitor of 20S proteasome. Cerpegin can be used as a tranquillizer, anti-inflammatory, analgesic and antiulcer .

HY-N0375

18α-Glycyrrhetinic acid	Triterpenes Structural Classification Neurological Disease Classification of Application Fields Leguminosae Terpenoids Source classification Plants Glycyrrhiza uralensis Fisch. Inflammation/Immunology Disease Research Fields	Proteasome NF-κB Apoptosis
18α-Glycyrrhetinic acid, a diet-derived compound, is an inhibitor of NF-kB and an activator of *proteasome, which serves as pro-longevity and anti-aggregation factor in a multicellular organism. 18α-Glycyrrhetinic acid induces apoptosis* .

HY-N2117R

Isoginkgetin (Standard)	Structural Classification Flavonoids Ginkgoaceae Source classification Phenols Polyphenols Plants Biflavones Ginkgo biloba	MMP Akt NF-κB Proteasome Apoptosis Autophagy
Isoginkgetin (Standard) is the analytical standard of Isoginkgetin. This product is intended for research and analytical applications. Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy .

HY-N2166

Tomatine α-Tomatine; Lycopersicin; Tomatin	Structural Classification Source classification Solanum lycopersicum L. Solanaceae Plants Steroids	Proteasome Apoptosis
Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity .

HY-N0415

Trigonelline chloride 4 Publications Verification Trigonelline hydrochloride	Infection Alkaloids Structural Classification Classification of Application Fields Labiatae Source classification Pyridine Alkaloids Metabolic Disease Lactuca perennis Plants Disease Research Fields	Endogenous Metabolite Ferroptosis Apoptosis HIV Bacterial Fungal
Trigonelline chloride is an alkaloid with potential antidiabetic activity that can be isolated from Trigonella foenum-graecum L or Leonurus artemisia. Trigonelline chloride is a potent Nrf2 inhibitor that blocks Nrf2-dependent proteasome activity, thereby enhancing apoptosis in pancreatic cancer cells. Trigonelline chloride also has anti-HSV-1, antibacterial, and antifungal activity, and induces ferroptosis.

HY-N0414

Trigonelline 4 Publications Verification Trigenolline	Structural Classification Classification of Application Fields Source classification Pyridine Alkaloids Metabolic Disease Plants Endogenous metabolite Alkaloids Microorganisms other families Leguminosae Trigonella foenum-graecum Linn. Disease Research Fields	Endogenous Metabolite Ferroptosis Apoptosis HIV Bacterial Fungal
Trigonelline is an alkaloid with potential antidiabetic activity that can be isolated from Trigonella foenum-graecum L or Leonurus artemisia. Trigonelline is a potent Nrf2 inhibitor that blocks Nrf2-dependent proteasome activity, thereby enhancing apoptosis in pancreatic cancer cells. Trigonelline also has anti-HSV-1, antibacterial, and antifungal activity and induces ferroptosis.

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-N0375R

18α-Glycyrrhetinic acid (Standard)	Triterpenes Structural Classification Leguminosae Terpenoids Source classification Plants Glycyrrhiza uralensis Fisch.	Proteasome NF-κB Apoptosis
18α-Glycyrrhetinic acid (Standard) is the analytical standard of 18α-Glycyrrhetinic acid. This product is intended for research and analytical applications. 18α-Glycyrrhetinic acid, a diet-derived compound, is an inhibitor of NF-kB and an activator of proteasome, which serves as pro-longevity and anti-aggregation factor in a multicellular organism. 18α-Glycyrrhetinic acid induces apoptosis .

HY-N7056

4'-Hydroxychalcone	Structural Classification Classification of Application Fields Source classification Plants Endogenous metabolite Chalcones Monophenols Flavonoids Leguminosae Phenols Inflammation/Immunology Disease Research Fields Glycyrrhiza uralensis Fisch.	Oxidative Phosphorylation Proteasome
4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via *proteasome* inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria .

HY-16594

Lactacystin 3 Publications Verification	Structural Classification Microorganisms Antibiotics Source classification Other Antibiotics	Proteasome Apoptosis ROS Kinase
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S *proteasome* inhibitor (IC₅₀ = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on ^[1] ^[2] ^[3] ^[4] ^[5] ^[6] ^[7] ^[8] ^[9] ^[10].

HY-N0414R

Trigonelline (Standard)	Alkaloids Structural Classification Microorganisms other families Leguminosae Source classification Pyridine Alkaloids Plants Endogenous metabolite Trigonella foenum-graecum Linn.	Endogenous Metabolite Ferroptosis Apoptosis HIV Bacterial Fungal
Trigonelline (Standard) is the analytical standard of Trigonelline. This product is intended for research and analytical applications. Trigonelline is an alkaloid with potential antidiabetic activity that can be isolated from Trigonella foenum-graecum L or Leonurus artemisia. Trigonelline is a potent Nrf2 inhibitor that blocks Nrf2-dependent proteasome activity, thereby enhancing apoptosis in pancreatic cancer cells. Trigonelline also has anti-HSV-1, antibacterial, and antifungal activity and induces ferroptosis.

HY-N0415R

Trigonelline chloride (Standard)	Alkaloids Structural Classification Labiatae Source classification Pyridine Alkaloids Lactuca perennis Plants	Endogenous Metabolite Ferroptosis Apoptosis HIV Bacterial Fungal
Trigonelline (chloride) (Standard) is the analytical standard of Trigonelline (chloride). This product is intended for research and analytical applications. Trigonelline chloride is an alkaloid with potential antidiabetic activity that can be isolated from Trigonella foenum-graecum L or Leonurus artemisia. Trigonelline chloride is a potent Nrf2 inhibitor that blocks Nrf2-dependent proteasome activity, thereby enhancing apoptosis in pancreatic cancer cells. Trigonelline chloride also has anti-HSV-1, antibacterial, and antifungal activity, and induces ferroptosis.

HY-N0060B

(E)-Ferulic acid (E)-Coniferic acid	Structural Classification Classification of Application Fields Source classification Plants Endogenous metabolite Human Gut Microbiota Metabolites Monophenols Microorganisms other families Simple Phenylpropanols Phenols Phenylpropanoids Disease Research Fields Cancer	β-catenin Bcl-2 Family Ferroptosis Endogenous Metabolite
(E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.

HY-N0060BR

(E)-Ferulic acid (Standard)	Structural Classification Human Gut Microbiota Metabolites Monophenols Microorganisms other families Simple Phenylpropanols Source classification Phenols Phenylpropanoids Plants Endogenous metabolite	β-catenin Bcl-2 Family Ferroptosis Endogenous Metabolite
(E)-Ferulic acid (Standard) is the analytical standard of (E)-Ferulic acid. This product is intended for research and analytical applications. (E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.

Cat. No.	Product Name	Chemical Structure

HY-10227S

Bortezomib-d8
Bortezomib-d₈ is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].

HY-10455S

Carfilzomib-d8
Carfilzomib-d₈ is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks