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Allen proteasome Inhibitors

" in MedChemExpress (MCE) Product Catalog:

187

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7

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1

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20

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3

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14

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19

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2

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-157032

    Proteasome Others
    Proteasome-IN-5 (compound 5) is a proteasome inhibitor .
    <em>Proteasome</em>-IN-5
  • HY-134961

    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 .
    Z-Ala-Arg-Arg-AMC
  • HY-144369

    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 .
    <em>Proteasome</em>-IN-4
  • HY-150591

    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 <em>Proteasome</em>-IN-3
  • HY-157035

    Proteasome Others
    Proteasome β2c/i-IN-1 (compound 37) is a subunit-selective human proteasome β2c and β2i inhibitor .
    <em>Proteasome</em> β2c/i-IN-1
  • HY-151195

    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 <em>Proteasome</em>-IN-4
  • HY-150590

    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 <em>Proteasome</em>-IN-2
  • HY-P3414A
    Proteasome-activating peptide 1 TFA
    1 Publications Verification

    Proteasome Neurological Disease
    Proteasome-activating peptide 1 TFA is a peptide and a potent proteasome activator. Proteasome-activating peptide 1 TFA increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 TFA prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis .
    <em>Proteasome</em>-activating peptide 1 TFA
  • HY-100172

    Proteasome Cancer
    Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1.
    <em>Proteasome</em>-IN-1
  • HY-139331

    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 <em>Proteasome</em>-IN-1
  • HY-157212

    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 .
    PARP-1/<em>Proteasome</em>-IN-1
  • HY-107412

    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 .
    <em>Proteasome</em> inhibitor IX
  • HY-150602

    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 <em>Proteasome</em> activator 1
  • HY-P10060

    Biochemical Assay Reagents Others
    Boc-Val-Gly-Arg-AMC is a peptide substrate that can be used to study activity of the proteasome .
    Boc-Val-Gly-Arg-AMC
  • HY-P10003

    Proteasome Cancer
    iso-VQA-ACC is a substrate for constitutive proteasome .
    iso-VQA-ACC
  • HY-P10003A

    Proteasome Others
    iso-VQA-ACC TFA is a constitutive proteasome substrate .
    iso-VQA-ACC TFA
  • HY-P1258

    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 .
    PSI
  • HY-135396

    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-137281

    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 .
    HMB-Val-Ser-Leu-VE
  • HY-149514

    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-153582

    PROTACs Bcr-Abl Cancer
    ML 2-23 is a potent PROTAC BCR-ABL degrader. ML 2-23 is selectively degrade BCR-ABL in a proteasome-dependent manner in leukemia cells .
    ML 2-23
  • HY-P2016

    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 .
    Ac-Nle-Pro-Nle-Asp-AMC
  • HY-129867

    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-123053

    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-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-137286

    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-144980

    Ligands for E3 Ligase Cancer
    E3 ligase Ligand 21 (compound 2) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .
    E3 ligase Ligand 21
  • HY-144983

    Ligands for E3 Ligase Cancer
    E3 ligase Ligand 22 (compound 139) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .
    E3 ligase Ligand 22
  • HY-155103

    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 .
    Antitrypanosomal agent 15
  • HY-144985

    Ligands for E3 Ligase Cancer
    E3 ligase Ligand 23 (compound 17-6) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .
    E3 ligase Ligand 23
  • HY-153034

    Others Cancer
    LONP1-IN-2 (compound 9d) is a potent and selective LONP1 inhibitor with IC50 values of 0.187 μM and >10 μM for LONP1 and 20S proteasome, respectively. LONP1-IN-2 can be used in research of cancer .
    LONP1-IN-2
  • HY-13259D

    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)
  • HY-123051

    Proteasome Inflammation/Immunology
    Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .
    Ac-WLA-AMC
  • HY-12113

    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 .
    Oprozomib
  • 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 .
    MG-132
  • HY-P4284

    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 .
    Z-GGF-CMK
  • HY-160289

    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 .
    ARI-3144
  • HY-127102

    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 .
    GSK3494245
  • HY-P1258A

    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 .
    PSI TFA
  • HY-10454
    Delanzomib
    1 Publications Verification

    CEP-18770

    Proteasome NF-κB Apoptosis Cancer
    Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities .
    Delanzomib
  • HY-N10332

    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 .
    Leptosphaerodione
  • HY-136563

    Proteasome Apoptosis Reactive Oxygen Species Cancer
    RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead .
    RA375
  • HY-120060

    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 .
    GNF6702
  • 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-W017227

    Proteasome Metabolic Disease
    Alloxan hydrate is a diabetogenic agent to induce diabetes. Alloxan hydrate is a proteasome inhibitor. Alloxan causes diabetes in experimental animals through its ability to destroy the insulin-secreting B-cells of the pancreas .
    Alloxan hydrate
  • HY-141543

    β-catenin Cancer
    YW2065 is an Axin-1 stabilizer. Axin-1 is a scaffolding protein that regulates proteasome degradation of β-catenin. YW2065 exhibits anti-colorectal cancer effects via dual activities of wnt/β-catenin signaling inhibition and AMPK activation .
    YW2065
  • HY-19934A

    TAS-117 hydrochloride

    Akt Apoptosis Autophagy Cancer
    Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy .
    Pifusertib hydrochloride
  • HY-19934

    TAS-117

    Akt Apoptosis Autophagy Cancer
    Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy .
    Pifusertib
  • HY-155643

    PROTACs Glutaminase Cancer
    PROTAC TG2 degrader-1 (compound 11) is a von Hippel-Lindau (VHL)-based PROTAC targeting tissue transglutaminase (TG2) with a KD of 68.9 μM. PROTAC TG2 degrader-1 reduces TG2 in ovarian cancer cells in a proteasome-dependent manner .
    PROTAC TG2 degrader-1
  • HY-144452

    Proteasome Cancer
    Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the research of certain neoplastic diseases .
    Immunoproteasome inhibitor 1

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