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Results for "

Proteasome subunits

" in MedChemExpress (MCE) Product Catalog:

27

Inhibitors & Agonists

1

Fluorescent Dye

3

Peptides

1

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 .
    GSK3494245
  • 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-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-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-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 . (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-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-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-168902
    Proteasome-IN-7

    		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 β2c/i-IN-1

    		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-IN-6

    		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-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 .
    PR-39
  • 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 .
    PR-39 TFA
  • HY-157034
    LU-002i

    		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-157034A
    LU-002i TFA

    		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
    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-162965
    Immunoproteasome activator 1

    		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-13821
    Epoxomicin
    10+ 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-123051
    Ac-WLA-AMC

    		Proteasome Inflammation/Immunology
    Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .
    Ac-WLA-AMC
  • HY-159808
    TCL1

    		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-114170
    ML604440
    2 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
    RA375

    		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-114419
    Zetomipzomib

    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
    1 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-149127
    Rosolutamide

    ASC-JM17; ALZ-003

    		 Keap1-Nrf2 Androgen Receptor HSP Mitophagy Metabolic Disease
    Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby activating the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels .
    Rosolutamide
  • HY-160876
    BC-1901S

    		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-13207
    ONX-0914
    Maximum Cited Publications
    17 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-13207A
    ONX-0914 TFA
    Maximum Cited Publications
    17 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

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