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20S proteasomes

" in MedChemExpress (MCE) Product Catalog:

51

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1

Fluorescent Dye

7

Peptides

8

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1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-123053
    Z-Leu-Leu-Glu-AMC

    Z-LLE-AMC

    		 Proteasome Others
    Z-Leu-Leu-Glu-AMC is a substrate peptide, and can be used for determination of postacidic-like hydrolysing activity of 20S proteasome
    Z-Leu-Leu-Glu-AMC
  • HY-120722
    TCH-165
    1 Publications Verification

    		 Proteasome Cancer
    TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation .
    TCH-165
  • HY-123051
    Ac-WLA-AMC

    		Proteasome Inflammation/Immunology
    Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .
    Ac-WLA-AMC
  • 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
  • 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) .
    20S Proteasome-IN-4
  • 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 .
    20S Proteasome-IN-2
  • 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 .
    Z-Leu-Leu-Leu-AMC
  • HY-169144
    Bortezomib analog

    		Proteasome Cancer
    Bortezomib analog (Compound 13), an analog of Bortezomib (HY-10227), is an active control of 20S proteasome subunit β5 ligand.
    Bortezomib analog
  • 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 .
    Z-Leu-Leu-Glu-βNA
  • HY-115391
    Boc-LRR-AMC

    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 .
    Boc-LRR-AMC
  • HY-153034
    LONP1-IN-2

    		Others Cancer
    LONP1-IN-2 (compound 9e) is a potent and selective LONP1 inhibitor with IC50 values of 0.093 μM and >10 μM for LONP1 and 20S proteasome, respectively. LONP1-IN-2 can be used in research of cancer .
    LONP1-IN-2
  • 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 .
    PROTAC 20S proteasome subunit β5 degrader 2
  • HY-150602
    20S Proteasome activator 1

    		Proteasome Neurological Disease
    20S Proteasome activator 1 is a potent 20S proteasome activator with EC200 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases .
    20S Proteasome activator 1
  • 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 .
    20S Proteasome-IN-5
  • 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 .
    20S Proteasome-IN-1
  • 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 .
    RAMB4
  • HY-169134
    PROTAC 20S proteasome subunit β5 degrader 1

    		PROTACs Apoptosis Cancer
    PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) is a targeted degrader of PROTAC for 20S proteasome subunit β5, with a DC50 value of 0.11 μM in FaDu cells. PROTAC 20S proteasome subunit β5 degrader 1 disrupts the cell cycle, promotes apoptosis, and inhibits cell proliferation and migration in both FaDu and KM3/BTZ cells. PROTAC 20S proteasome subunit β5 degrader 1 can be used to study the resistance of pharyngeal cancer and multiple myeloma to Bortezomib (HY-10227) (Pink: Target protein ligand (HY-10227); Blue: E3 ligase ligand (HY-103596); Black: Linker (HY-169142)) .
    PROTAC 20S proteasome subunit β5 degrader 1
  • HY-108549
    clasto-Lactacystin β-lactone

    Omuralide; β-Clastolactacystin

    		 Proteasome Cancer
    Clasto-Lactacystin β-lactone, a natural active metabolite of lactacystin, which is a metabolite of Streptomyces, acts as an irreversible 20S proteasome inhibitor.
    clasto-Lactacystin β-lactone
  • 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 (Ki of 0.93 nM).
    Ixazomib
  • HY-10452
    Ixazomib citrate
    5 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 Ki of 0.93 nM.
    Ixazomib citrate
  • HY-123052
    Ac-PAL-AMC

    		Proteasome Inflammation/Immunology
    Ac-PAL-AMC is a fluorogenic substrate specific for 20S proteasome LMP2/β1i activity .
    Ac-PAL-AMC
  • HY-163770
    Anticancer agent 233

    		Proteasome Cancer
    Anticancer agent 233 (compound 5g) is a 3,5-bis(arylmethylene)-4-piperidinone derivative with anticancer activity, with GI50 of 0.25 and 0.23 μM for cervical cancer (HeLa) and colon cancer (HCT116) cell lines, respectively. The chlorine atom on the aromatic ring of Anticancer agent 233 interacts well with the catalytic site of 20S proteasome, inhibiting the activity of 20S proteasome to exert its anticancer effect .
    Anticancer agent 233
  • HY-135511
    Nor-Cerpegin

    		Proteasome Inflammation/Immunology
    Nor-Cerpegin (Cerpegin), a pyridinone-fused c-lactone, is an inhibitor of 20S proteasome. Nor-Cerpegin (Cerpegin) can be used as a tranquillizer, anti-inflammatory, analgesic and antiulcer .
    Nor-Cerpegin
  • 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.
    Celastrol (Standard)
  • HY-108552
    MG-115
    1 Publications Verification

    		 Proteasome Apoptosis Cancer
    MG-115 is a potent and reversible proteasome inhibitor, with Kis 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 .
    MG-115
  • HY-169158
    Bortezomib analog 1

    		Ligands for Target Protein for PROTAC Cancer
    Bortezomib analog 1 is an analog of Bortezomib (HY-10227). Bortezomib analog 1 and can be used to synthesize PROTAC 20S proteasome subunit β5 degrader 1 (HY-169134) .
    Bortezomib analog 1
  • 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 .
    RID-F
  • 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 (Ki of 0.93 nM).
    Ixazomib (Standard)
  • HY-10227
    Bortezomib
    Maximum Cited Publications
    145 Publications Verification

    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 (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 .
    Bortezomib
  • 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 .
    Isoginkgetin
  • 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 .
    Proteasome inhibitor IX
  • 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 .
    BC-05
  • 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 .
    Boc-LRR-AMC TFA
  • HY-108553
    Dihydroeponemycin

    		Proteasome Apoptosis Cancer
    Dihydroeponemycin, an analogue of the antitumor and antiangiogenic natural product eponemycin, selectively targets the 20S proteasome. Dihydroeponemycin covalently modifies a subset of catalytic proteasomal subunits, binding preferentially to the IFN-gamma-inducible subunits LMP2 and LMP7. Dihydroeponemycin-mediated proteasome inhibition induces a spindle-like cellular morphological change and apoptosis .
    Dihydroeponemycin
  • HY-150226
    Enzyme-IN-1

    		Proteasome Inflammation/Immunology
    Enzyme-IN-1 (compound 1) is a peptide-based inhibitor of N-terminal nucleophile (Ntn) hydrolases. Specifically, Enzyme-IN-1 inhibits the chymotrypsin-like activity (CT-L) of the 20S proteasome. Enzyme-IN-1 may has potential antiinflammatory properties .
    Enzyme-IN-1
  • HY-N2166
    Tomatine

    α-Tomatine; Lycopersicin; Tomatin

    		 Proteasome Apoptosis Neurological Disease
    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 .
    Tomatine
  • HY-N2166A
    Tomatine hydrochloride

    α-Tomatine hydrochloride; Lycopersicin hydrochloride; Tomatin hydrochloride

    		 Proteasome Apoptosis Neurological Disease
    Tomatine hydrochloride is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine hydrochloride elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine hydrochloride promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine hydrochloride also inhibits 20S proteasome activity .
    Tomatine hydrochloride
  • 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 (Ki 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 .
    (1S,2S)-Bortezomib
  • 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].
    Bortezomib-d8
  • 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) .
    Marizomib
  • 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 (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 .
    Bortezomib (Standard)
  • HY-N2117R
    Isoginkgetin (Standard)

    		MMP Akt NF-κB Proteasome Apoptosis Autophagy Inflammation/Immunology Cancer
    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 .
    Isoginkgetin (Standard)
  • 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 .
    Celastrol
  • 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 .
    Cadmium pyrithione
  • HY-136528
    RA-9

    		Deubiquitinase Apoptosis Cancer
    RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells .
    RA-9
  • HY-126874
    Tyropeptin A-4

    TP-101

    		 Others Others
    Tyropeptin A-4 (TP-101) is a potent proteasome inhibitor with the ability to inhibit mammalian 20S proteasome activity. Tyropeptin A-4 exerts its inhibitory effect by binding to the site responsible for trypsin-like activity. Tyropeptin A-4 derivative TP-104 has a 20-fold increase in inhibitory activity over Tyropeptin A. TP-110 specifically inhibits trypsin-like activity without affecting PGPH and trypsin-like activity .
    Tyropeptin A-4
  • HY-16594
    Lactacystin
    3 Publications Verification

    		 Proteasome Apoptosis ROS Kinase Infection Cardiovascular Disease Neurological Disease Cancer
    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] .
    Lactacystin
  • HY-139062
    C6 Urea Ceramide

    C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide

    		 Others Cancer
    C6 Urea Ceramide (C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells, but not in MEFs lacking neutral ceramidase. At concentrations of 5 and 10 μM, it inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but not in noncancerous RIE-1 cells. C6 Urea Ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the 20S proteasome in HT-29 and HCT116 cells, but not in RIE-1 cells. When administered at doses of 1.25, 2.5, and 5 mg/kg for five days, it reduces tumor growth and increases C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
    C6 Urea Ceramide
  • HY-161079
    TDI-8304

    		Parasite Infection
    TDI-8304, a macrocyclic peptide, is a potent, species selective, and noncovalent Plasmodium falciparum (Pf20S) inhibitor. TDI-8304 shows highly selective for Pf20S over human proteasomes .
    TDI-8304
  • HY-W940797
    Thalidomide-O-amido-C7-NH2

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide-O-amido-C7-NH2 is a E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACT .
    Thalidomide-O-amido-C7-NH2

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