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Results for "

Proteasome inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Proteasome (67) Akt (3) Androgen Receptor (1) Apoptosis (30) Autophagy (14) Bacterial (6) Bcl-2 Family (1) BCL6 (1) c-Met/HGFR (1) Calcium Channel (1) Caspase (1) ClpP (1) Deubiquitinase (6) DNA/RNA Synthesis (1) Drug-Linker Conjugates for ADC (1) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (1) EGFR (3) Endogenous Metabolite (3) Epigenetic Reader Domain (1) Ferroptosis (2) FLT3 (1) Fungal (2) HDAC (2) Hexokinase (1) Histone Methyltransferase (3) HIV (4) IKK (1) Isotope-Labeled Compounds (1) Keap1-Nrf2 (1) Mitophagy (1) MMP (1) NAMPT (2) NF-κB (8) NOD-like Receptor (NLR) (1) Oxidative Phosphorylation (1) p97 (1) Parasite (7) PARP (2) PERK (1) PROTACs (7) RAD51 (1) Raf (1) Reactive Oxygen Species (1) Ribosomal S6 Kinase (RSK) (1) ROS Kinase (1) Ser/Thr Protease (1) SNIPERs (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (82) Cardiovascular Disease (2) Infection (13) Inflammation/Immunology (20) Metabolic Disease (5) Neurological Disease (5)

By Targets:

Proteasome (67)

Akt (3)

Androgen Receptor (1)

Apoptosis (30)

Autophagy (14)

Bacterial (6)

Bcl-2 Family (1)

BCL6 (1)

c-Met/HGFR (1)

Calcium Channel (1)

Caspase (1)

ClpP (1)

Deubiquitinase (6)

DNA/RNA Synthesis (1)

Drug-Linker Conjugates for ADC (1)

E1/E2/E3 Enzyme (1)

E3 Ligase Ligand-Linker Conjugates (1)

EGFR (3)

Endogenous Metabolite (3)

Epigenetic Reader Domain (1)

Ferroptosis (2)

FLT3 (1)

Fungal (2)

HDAC (2)

Hexokinase (1)

Histone Methyltransferase (3)

HIV (4)

IKK (1)

Isotope-Labeled Compounds (1)

Keap1-Nrf2 (1)

Mitophagy (1)

MMP (1)

NAMPT (2)

NF-κB (8)

NOD-like Receptor (NLR) (1)

Oxidative Phosphorylation (1)

p97 (1)

Parasite (7)

PARP (2)

PERK (1)

PROTACs (7)

RAD51 (1)

Raf (1)

Reactive Oxygen Species (1)

Ribosomal S6 Kinase (RSK) (1)

ROS Kinase (1)

Ser/Thr Protease (1)

SNIPERs (1)

Wnt (1)

β-catenin (1)

By Research Areas:

Cancer (82)

Cardiovascular Disease (2)

Infection (13)

Inflammation/Immunology (20)

Metabolic Disease (5)

Neurological Disease (5)

111

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 .

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-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-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-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.

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

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

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-13067

Celastrol 30+ Cited Publications Tripterine; Tripterin	Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite	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.

HY-10227

Bortezomib 115+ 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-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-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-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 .

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 10+ 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 .

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-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-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-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-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-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-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 .

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

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-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-12471

VLX1570

2 Publications Verification

Deubiquitinase Cancer

VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC₅₀ of approximate 10 μM.

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 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

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 .

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

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-10455

Carfilzomib 20+ 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 .

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

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-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-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-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-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-131350

LXE408	Proteasome Parasite	Infection
LXE408 is an orally active, non-competitive and kinetoplastid-selective *proteasome* inhibitor. LXE408 has an IC₅₀ of 0.04 μM for *L. donovani* proteasome and an EC₅₀ of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research .

HY-13821

Epoxomicin 5+ Cited Publications BU-4061T	Proteasome Apoptosis	Inflammation/Immunology Cancer
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-120060

GNF6702	Parasite	Infection
GNF6702 is a selective inhibitor of the kinetoplastid proteasome. GNF6702 clears parasites in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis .

HY-13259

MG-132 Maximum Cited Publications 872 Publications Verification Z-Leu-Leu-Leu-al; MG132	Proteasome Autophagy Apoptosis	Cancer
MG-132 (Z-Leu-Leu-Leu-al) is a potent *proteasome* and calpain inhibitor with IC₅₀s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis .

HY-10452

Ixazomib citrate 4 Publications Verification MLN9708	Proteasome Autophagy	Cancer
Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC₅₀ of 3.4 nM and a K_i of 0.93 nM.

HY-156105

8304-vs	Parasite Proteasome	Infection
8304-vs is a macrocyclic anti-Plasmodial agent that covalently and irreversibly targets the Plasmodium proteasome. 8304-vs effectively inhibits the growth of Plasmodium falciparum .

HY-10455S

Carfilzomib-d8	Isotope-Labeled Compounds Proteasome Autophagy Apoptosis	Cancer
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.

HY-N2117

Isoginkgetin 10+ Cited Publications	MMP Akt NF-κB Proteasome Apoptosis Autophagy	Inflammation/Immunology Cancer
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-138284

Avenanthramide-C methyl ester	NF-κB	Inflammation/Immunology
Avenanthramide-C methyl ester is an anti-inflammatory agent and NF-κB inhibitor that inhibits the secretion of pro-inflammatory factors. Avenanthramide-C methyl ester inhibits NF-κB activation by inhibiting IKK and IκB phosphorylation and inhibiting proteasome activity .

Cat. No.	Product Name

HY-L012

Metabolism/Protease Compound Library

4431 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 4431 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.

HY-L050

Ubiquitination Compound Library

286 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 286 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

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

88 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 88 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-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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13067

Celastrol Maximum Cited Publications 31 Publications Verification Tripterine; Tripterin	Triterpenes Structural Classification Classification of Application Fields Anti-aging Terpenoids Source classification Celastraceae Plants Tripterygium wilfordii Hook. f. Inflammation/Immunology Disease Research Fields Cancer	Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite
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-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-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-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-13821

Epoxomicin 5+ Cited Publications BU-4061T	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-N0375

18α-Glycyrrhetinic acid	Triterpenes Classification of Application Fields Neurological Disease Leguminosae Terpenoids Source classification Plants Disease Research Fields Inflammation/Immunology Glycyrrhiza uralensis Fisch.	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-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 other families Microorganisms Leguminosae Disease Research Fields Trigonella foenum-graecum Linn.	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-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 2 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].

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.

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