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Results for "

proteasome substrate

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Proteasome (15) Apoptosis (3) ATP Synthase (1) Autophagy (2) Bcl-2 Family (1) Biochemical Assay Reagents (3) Caspase (1) Deubiquitinase (2) FAP (1) Histone Methyltransferase (3) IKZF Family (1) MDM-2/p53 (1) Molecular Glues (1) NF-κB (1) PARP (1) PROTACs (3) Ser/Thr Protease (1)
By Research Areas:	Cancer (10) Cardiovascular Disease (1) Endocrinology (1) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Peptides

Targets Recommended: Proteasome MARCKS Proteasome Cap Targeting Chimeras

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13817

IU1 Maximum Cited Publications 25 Publications Verification	Deubiquitinase Autophagy Apoptosis	Cardiovascular Disease Neurological Disease Endocrinology Cancer
IU1 is a selective, reversible USP14 inhibitor with an IC₅₀ of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .

HY-123053

Z-Leu-Leu-Glu-AMC 3 Publications Verification Z-LLE-AMC	Proteasome	Neurological Disease
Z-Leu-Leu-Glu-AMC (Z-LLE-AMC) is a peptide-AMC linked substrate used to measure the postacidic-like hydrolysing activity of *proteasome*. Z-Leu-Leu-Glu-AMC can be used for the research of parkinson's disease .

HY-115391

Boc-LRR-AMC 1 Publications Verification Boc-Leu-Arg-Arg-AMC	Biochemical Assay Reagents	Others
Boc-LRR-AMC (Boc-Leu-Arg-Arg-AMC) is a fluorogenic substrate, which can be utilized for detecting the trypsin-like activity of the 26S proteasome or the 20S proteasome core .

HY-123051

Ac-WLA-AMC	Proteasome	Inflammation/Immunology
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .

HY-12286

PI-1840	Proteasome Apoptosis Autophagy Caspase Bcl-2 Family NF-κB PARP	Cancer
PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC₅₀ value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α .

HY-135070

Ac-RLR-AMC Ac-Arg-Leu-Arg-AMC	Proteasome	Others
Ac-RLR-AMC (Ac-Arg-Leu-Arg-AMC) is a fluorogenic substrate for the 26S proteasome (Ex/Em: 380/440-460 nm). AMC is released upon cleavage, and its fluorescence can be used to quantify the trypsin-like activity of 26S proteasomes .

HY-160289

ARI-3144	FAP	Cancer
ARI-3144 is an excellent and specific substrate for fibroblast activation protein (FAP). ARI-3144 is usually coupled with the fluorophore 7-Amino-4-methylcoumarin (HY-D0027) (AMC) for detection and quantification of FAP .

HY-123052

Ac-PAL-AMC	Proteasome	Inflammation/Immunology
Ac-PAL-AMC is a fluorogenic substrate specific for 20S proteasome LMP2/β1i activity .

HY-134961

Z-Ala-Arg-Arg-AMC 1 Publications Verification Fluorogenic proteasome substrate; Z-ARR-AMC	Proteasome	Others
Z-Ala-Arg-Arg-AMC (Fluorogenic Proteasome Substrate) is a fluorogenic substrate for assaying trypsin-like activity of proteasome .

HY-W012985

Methyl pyruvate	ATP Synthase Apoptosis	Metabolic Disease Cancer
Methyl pyruvate is a methyl ester derivative of pyruvic acid. Methyl pyruvate induces insulin release and membrane depolarization. Methyl pyruvate rescues proteasome damage and nuclear localization of TdP-43 caused by overexpression of σ1RE102Q by enhancing ATP synthesis. Methyl pyruvate selectively protects normal lung fibroblasts from cell death induced by Irinotecan (HY-16562). Methyl pyruvate promotes apoptosis and necrosis in cancer cells and downregulates angiogenesis and cell cycle pathways. Methyl pyruvate is an effective substrate for dihydrodihydrogen dehydrogenase.

HY-129867

Z-Leu-Leu-Leu-AMC Z-LLL-AMC	Proteasome	Others
Z-Leu-Leu-Leu-AMC is a fluorogenic substrate for measuring the chymotrypsin-like protease activity of the 20S proteasome .

HY-P2016

Ac-Nle-Pro-Nle-Asp-AMC	Proteasome	Others
Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate for 26S proteasome. Ac-Nle-Pro-Nle-Asp-AMC can be used for the 26S proteasome caspase-like activity analysis .

HY-156152A

CARM1 degrader-1 hydrochloride	PROTACs Histone Methyltransferase	Cancer
CARM1 degrader-1 hydrochloride is a CARM1 PROTAC degrader (DC₅₀ = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 hydrochloride degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 hydrochloride downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 hydrochloride inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 hydrochloride can be used in breast cancer research .

HY-P5280

Ac-KQL-AMC	Ser/Thr Protease	Others
Ac-KQL-AMC is a fluorogenic substrate that can be used to quantify Trypsin-like activity, resulting in detectable fluorescence when cleaved by the proteasome .

HY-137286

Z-Leu-Leu-Glu-βNA Z-Leu-Leu-Glu-β-naphthylamide	Proteasome	Others
Z-Leu-Leu-Glu-βNA (Z-Leu-Leu-Glu-β-naphthylamide) is a substrate for determination of the glutamylpeptidyl-peptide hydrolase activity of the 20S proteasome .

HY-P10003B

iso-VQA-ACC acetate	Proteasome	Others
iso-VQA-ACC acetate is a substrate for constitutive proteasome .

HY-156152

CARM1 degrader-1	PROTACs Histone Methyltransferase	Cancer
CARM1 degrader-1 is a CARM1 PROTAC degrader (DC₅₀ = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 can be used for the research of breast cancer .

HY-137897

Bz-VGR-AMC	Proteasome	Others
Bz-VGR-AMC is a substrate for the trypsin-like activity of the 20S proteasome. Bz-VGR-AMC can be used to measure the trypsin-like (β2) activity of the 20S proteasome .

HY-174266

WB156	MDM-2/p53	Cancer
WB156 is a dual MDM2 and GSPT1 degrader. WB156 can recruit CRBN (Cereblon, a substrate receptor of the E3 ubiquitin-ligase complex) to induce the ubiquitination-proteasome pathway-mediated degradation of MDM2 and GSPT1. WB156 is promising for research of cancers, such as leukemia .

HY-P10003A

iso-VQA-ACC TFA	Proteasome	Others
iso-VQA-ACC TFA is a constitutive proteasome substrate .

HY-156153

CARM1 degrader-2	Histone Methyltransferase	Cancer
PROTAC CARM1 degrader-2 (compound 3e) is a degrader (DC₅₀=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-2 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-2 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .

HY-P10003

iso-VQA-ACC	Proteasome	Cancer
iso-VQA-ACC is a substrate for constitutive proteasome .

HY-P10060

Boc-Val-Gly-Arg-AMC	Biochemical Assay Reagents	Others
Boc-Val-Gly-Arg-AMC is a peptide substrate that can be used to study activity of the proteasome .

HY-P4514

Z-Gly-Gly-Arg-βNA	Proteasome	Others
Z-Gly-Gly-Arg-βNA is the synthetic peptide substrate of trypsin-like activities of the proteasome .

HY-135070B

Ac-RLR-AMC TFA Ac-Arg-Leu-Arg-AMC TFA	Proteasome	Others
Ac-RLR-AMC (Ac-Arg-Leu-Arg-AMC) TFA is a fluorogenic substrate for the 26S proteasome (Ex/Em: 380/440-460 nm). AMC is released upon cleavage, and its fluorescence can be used to quantify the trypsin-like activity of 26S proteasomes .

HY-W753820A

Boc-LRR-AMC TFA Boc-Leu-Arg-Arg-AMC TFA	Biochemical Assay Reagents	Others
Boc-LRR-AMC TFA (Boc-Leu-Arg-Arg-AMC TFA) is the TFA salt form of Boc-LRR-AMC (HY-115391). Boc-LRR-AMC TFA is a fluorogenic substrate, which can be utilized for detecting the trypsin-like activity of the 26S proteasome or the 20S proteasome core .

HY-135779

IU2-6	Deubiquitinase	Neurological Disease
IU2-6 is a USP14 deubiquitinase inhibitor. IU2-6 inhibits deubiquitinating activity of proteasome-associated USP14, blocks substrate rescue from degradation, and enhances proteasomal activity. IU2-6 can be used for the research of neurodegeneration .

HY-182799

IBA-12	PROTACs Molecular Glues IKZF Family	Cancer
IBA-12 is a IKZF2 molecular glue/PROTAC degrader with a DC₅₀ of 276.2 nM (Jurkat cells) and 461.8 nM (Mino cells), and an IC₅₀ of 179.9 nM. IBA-12 binds to the canonical tryptophan triad pocket of CRBN to form a ternary complex with IKZF2. IBA-12 induces IKZF2 degradation mediated by the CRBN-dependent ubiquitin-proteasome system, with no effect on other CRBN substrates. IBA-12 induces the production of interleukin-2 (IL-2) through degrading IKZF2. IBA-12 is applicable to cancer immunology research .

Cat. No.	Product Name

HY-L934

CRBN Ligand Library	125 compounds
CRBN, namely cereblon, is the substrate recognition subunit of the E3 ubiquitin ligase complex in the ubiquitin-proteasome system. A CRBN ligand library refers to a collection of numerous fragments that can specifically bind to the CRBN protein. These ligands are mostly designed based on validated CRBN-binding warheads and modified through AI-driven molecular generation optimization systems. They not only include classic lenalidomide-derived structures but also cover novel non-lenalidomide scaffolds. After drug-likeness filtering, these ligands exhibit structural diversity and favorable druggable properties. They can be further optimized and modified to facilitate the development of novel molecular glue degraders, accelerate the discovery of molecular glues that induce interactions between CRBN and new substrate proteins, and enable the exploration of novel CRBN substrates for identifying previously unknown CRBN-binding proteins. MCE compiles 125 fragments that can specifically bind to the CRBN protein, with molecular weights ranging from 200 to 500. Compounds developed based on the library ligands target multiple disease targets such as cancer and autoimmune diseases, further advancing the development of Molecular Glues and PROTACs therapeutic agents.

CRBN Ligand Library

125 compounds

CRBN, namely cereblon, is the substrate recognition subunit of the E3 ubiquitin ligase complex in the ubiquitin-proteasome system. A CRBN ligand library refers to a collection of numerous fragments that can specifically bind to the CRBN protein.

These ligands are mostly designed based on validated CRBN-binding warheads and modified through AI-driven molecular generation optimization systems. They not only include classic lenalidomide-derived structures but also cover novel non-lenalidomide scaffolds. After drug-likeness filtering, these ligands exhibit structural diversity and favorable druggable properties. They can be further optimized and modified to facilitate the development of novel molecular glue degraders, accelerate the discovery of molecular glues that induce interactions between CRBN and new substrate proteins, and enable the exploration of novel CRBN substrates for identifying previously unknown CRBN-binding proteins.

MCE compiles 125 fragments that can specifically bind to the CRBN protein, with molecular weights ranging from 200 to 500. Compounds developed based on the library ligands target multiple disease targets such as cancer and autoimmune diseases, further advancing the development of Molecular Glues and PROTACs therapeutic agents.

HY-L050

Ubiquitination Compound Library	482 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 482 small molecule modulators with biological activity used for ubiquitination research. Compounds in this library target the key enzymes in ubiquitin pathway. MCE Ubiquitination Compound Library is a useful tool for the research of ubiquitination regulation and the corresponding diseases.

Ubiquitination Compound Library

482 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 482 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.

Ac-WLA-AMC	Fluorescent Dye
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .

Cat. No.	Product Name	Target	Research Area