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proteasome subunit

" in MedChemExpress (MCE) Product Catalog:

37

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1

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1

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5

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1

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8

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19

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13821
    Epoxomicin
    20+ 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 .
    Epoxomicin
  • HY-13207
    ONX-0914
    Maximum Cited Publications
    24 Publications Verification

    PR-957

    Proteasome Bacterial HIV Infection Inflammation/Immunology
    ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .
    ONX-0914
  • HY-159607

    PROTACs SWI/SNF Complex Cancer
    PRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer .
    PRT3789
  • HY-P11307

    Proteasome Cancer
    Biotin-epoxomicin is a Proteasome subunit binder. Biotin-epoxomicin serves as an affinity reagent for identifying proteasomal catalytic subunits, and facilitates affinity purification of active proteasomal subunits for LC-MS identification. Biotin-epoxomicin can be used to study solid tumors derived from B16 melanoma .
    Biotin-epoxomicin
  • HY-P11306

    Proteasome NF-κB Inflammation/Immunology
    Biotin-(Oaa)3-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)3-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain .
    Biotin-(Oaa)3-epoxomicin
  • HY-123051

    Proteasome Inflammation/Immunology
    Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .
    Ac-WLA-AMC
  • HY-149127

    ASC-JM17; ALZ-003

    Keap1-Nrf2 Androgen Receptor HSP Mitophagy Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Autophagy Metabolic Disease
    Rosolutamide (ASC-JM17) is an orally active Nrf1/Nrf2 activator. Rosolutamide activates Hsf1 pathways, upregulates proteasome subunits and antioxidant enzymes, induces proteasome complex structural rearrangement, and enhances ubiquitin-proteasome system-mediated degradation. Rosolutamide reduces mutant androgen receptor and ataxin-3 aggregates, restores mitochondrial function, attenuates reactive oxygen species (ROS) levels, induces apoptosis and ferroptosis, and inhibits cancer cell growth. Rosolutamide can be used for the research of spinal and bulbar muscular atrophy, Huntington’s disease, and temozolomide-resistant glioblastoma .
    Rosolutamide
  • HY-114419
    Zetomipzomib
    4 Publications Verification

    KZR-616

    Proteasome Inflammation/Immunology
    Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases .
    Zetomipzomib
  • HY-114419A
    Zetomipzomib maleate
    4 Publications Verification

    KZR-616 maleate

    Proteasome Inflammation/Immunology
    Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases .
    Zetomipzomib maleate
  • HY-171705

    Keap1-Nrf2 AMPK JNK IKK p38 MAPK NO Synthase α-synuclein Interleukin Related Neurological Disease
    KMS99220 is an orally active, blood-brain barrier-permeable activator of the Nrf2 inhibitory protein Keap-1. KMS99220 enhances the activity of AMPK, activates the Nrf2 signaling pathway, and reduces the phosphorylation of IκB, nuclear translocation of NFκB, as well as the phosphorylation levels of JNK, IKK and p38 MAPK via HO-1. KMS99220 binds to Keap1 to trigger the nuclear translocation of Nrf2, induces the expression of HO-1, NQO1, GCLC, GCLM and proteasome subunits; enhances proteasomal enzymatic activity; inhibits iNOS expression, nitric oxide production and IL-1β generation; attenuates microglial activation; reduces α-synuclein aggregation; and prevents dopaminergic neuron degeneration and motor dysfunction. KMS99220 prevents the degeneration of dopaminergic neurons in the substantia nigra, induces the expression of Nrf2 downstream target genes, and effectively ameliorates associated motor dysfunction in a mouse model of Parkinson's disease. KMS99220 is applicable to research related to Parkinson's disease .
    KMS99220
  • HY-114170
    ML604440
    3 Publications Verification

    Proteasome Inflammation/Immunology
    ML604440 is a specific and cell-permeable Proteasome β1i (LMP2) subunit inhibitor. ML604440 can be used in experimental colitis, EAE and autoimmune disease research. ML604440 shows synergistic effects and advantageous when combined with LMP7 inhibitor .
    ML604440
  • HY-136563

    Proteasome Apoptosis Reactive Oxygen Species (ROS) 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-P1259A

    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 .
    PR-39 TFA
  • HY-162965

    Proteasome Cancer
    Immunoproteasome activator 1 (compound A) is a selective immunoproteasome activator that increases the presentation of individual MHC-I–bound peptides by over 100-fold. Immunoproteasome activator 1 binds to the proteasome structural subunit PSMA1 and promotes the association of the proteasome activator PA28α/β (PSME1/PSME2) with immunoproteasomes .
    Immunoproteasome activator 1
  • HY-13207A
    ONX-0914 TFA
    Maximum Cited Publications
    24 Publications Verification

    PR-957 TFA

    Proteasome Bacterial HIV Infection Inflammation/Immunology
    ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .
    ONX-0914 TFA
  • HY-157034
    LU-002i
    1 Publications Verification

    Proteasome Others
    LU-002i is a subunit-selective human proteasome β2c and β2i inhibitor with an IC50 value of 220 nM for β2i .
    LU-002i
  • 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-P1259

    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 .
    PR-39
  • HY-160876

    Keap1-Nrf2 E1/E2/E3 Enzyme Inflammation/Immunology
    BC-1901S is a proteasome-independent NRF2 activator and stabilizer. BC-1901S binds to DCAF1 (E3 ligase subunit) and disrupts NRF2/DCAF1 interaction, and activates NRF2 by inhibiting NRF2 ubiquitination in a KEAP1-independent manner. BC-1901S shows anti-inflammatory effect in a murine model of LPS-induced acute lung injury .
    BC-1901S
  • HY-169144

    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-169134

    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-170881

    Proteasome Cancer
    TIR-199 is a novel and highly specific dual proteasome inhibitor that can effectively inhibit the PSMB5 subunit of constitutive proteasome and the PSMB8 subunit of immunoproteasome. TIR-199 can induce the death of various tumor cells. TIR-199 can be used for research on myeloma .
    TIR-199
  • HY-159808

    Proteasome Cancer
    TCL1 is a selective non-covalent inhibitor targeting the Pru domain of the Rpn-13 subunit in the 19S regulatory particle (19S RP) of the proteasome with an IC50 value of approximately 26 μM. TCL1 interferes with the recognition and transport of ubiquitinated proteins by Rpn-13, inhibits the degradation of proteins by the proteasome, and thus affects the balance of intracellular protein metabolism. TCL1 is promising for research of hematological malignancies .
    TCL1
  • HY-169135

    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))
    PROTAC 20S proteasome subunit β5 degrader 2
  • 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 Proteasome-IN-2
  • HY-108553

    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-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 Proteasome-IN-3
  • HY-168902

    Proteasome Cancer
    Proteasome-IN-7 (Compound 6f) is an epoxyketone macrocyclic peptidyl proteasome inhibitor (IC50 value of 37.92 nM for 20S proteasome ChT-L subunit). Proteasome-IN-7 displays robust antiproliferative effects against multiple myeloma, acute lymphoblastic leukemia and non-small cell lung cancer .
    Proteasome-IN-7
  • HY-157035

    Proteasome Others
    Proteasome β2c/i-IN-1 (compound 37) is a subunit-selective human proteasome β2c and β2i inhibitor .
    Proteasome β2c/i-IN-1
  • HY-170363

    Proteasome Parasite Infection
    Proteasome-IN-6 (Compound J-80) inhibits the β5 catalytic subunit of the Trypanosoma brucei 20S proteasome, inibits T. b. brucei, T. b. gambiense and T. b. rhodesiense with EC50s of 157 nM, 220 nM and 156 nM, respectively. Proteasome-IN-6 exhibits antitrypanosomal activity in mouse model .
    Proteasome-IN-6
  • HY-157034A

    Proteasome Others
    LU-002i TFA is a subunit-selective human proteasome β2c and β2i inhibitor with an IC50 value of 220 nM for β2i .
    LU-002i TFA
  • HY-169158

    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-181495

    Proteasome Cap Targeting Chimeras PROTACs Proteasome Epigenetic Reader Domain Cancer
    RAJQ14 is a BRD4 PROTAC-like CAP-TAC (Proteasome Cap Targeting Chimeras) degrader. RAJQ14 binds to 19S proteasome cap subunits RPN1, RPN10, RPN13, and USP14 to recruit target proteins to the proteasome for ubiquitination-independent, proteasome-dependent degradation. RAJQ14 can be used for the research of cancer (Pink: BRD4 Ligand (HY-181496); Blue: Proteasome Ligand (HY-128978); Black: Linker).
    RAJQ14
  • HY-183009

    Proteasome Parasite Infection
    Pf20S-IN-1 is a selective inhibitor of the 20S proteasome β5 subunit of Plasmodium falciparum. Pf20S-IN-1 exhibits antiparasitic activity against Plasmodium falciparum, with an EC50 of 20.1 nM against the Plasmodium falciparum W2 strain. Pf20S-IN-1 shows weak inhibitory effect on human 20S proteasome, has no obvious toxicity to human foreskin fibroblasts (HFF), and has a selectivity index > 25000. Pf20S-IN-1 can be used in malaria research .
    Pf20S-IN-1
  • HY-181940

    Proteasome Cancer
    Berberine-amide-m-PhBA chloride (Compound 8b) is a selective anti-breast cancer agent. Berberine-amide-m-PhBA chloride may inhibit the proteasome by interacting with the 20S proteasome β5 subunit. Berberine-amide-m-PhBA chloride can be used in the research of breast cancer .
    Berberine-amide-m-PhBA chloride
  • HY-180538

    Molecular Glues E1/E2/E3 Enzyme Others
    MRT-31619 is a molecular gel degrader (MGD) targeting CRBN. MRT-31619 drives the self-dimerization of the E3 ligase by mimicking the degradation subunit, and promotes its rapid, effective and selective degradation through the ubiquitin-proteasome system .
    MRT-31619
  • HY-179499

    PROTACs Histone Methyltransferase Apoptosis Cancer
    PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research .
    PROTAC EZH2 Degrader-9

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