1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Proteasome

Proteasome

Proteasomes are very large protein complexes inside all eukaryotes and archaea, and in some bacteria. In eukaryotes, they are located in the nucleus and the cytoplasm. The main function of the proteasome is to degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Enzymes that carry out such reactions are called proteases. Proteasomes are part of a major mechanism by which cells regulate the concentration of particular proteins and degrade misfolded proteins. The degradation process yields peptides of about seven to eight amino acids long, which can then be further degraded into amino acids and used in synthesizing new proteins. Proteins are tagged for degradation with a small protein called ubiquitin. The tagging reaction is catalyzed by enzymes called ubiquitin ligases. Once a protein is tagged with a single ubiquitin molecule, this is a signal to other ligases to attach additional ubiquitin molecules. The result is a polyubiquitin chain that is bound by the proteasome, allowing it to degrade the tagged protein.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-137186
    Suc-Gly-Gly-Phe-pNA
    Suc-Gly-Gly-Phe-pNA is the chymotrypsin substrate with an Km value of 1.6 mM.
    Suc-Gly-Gly-Phe-pNA
  • HY-13067R
    Celastrol (Standard)
    Inhibitor
    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-113639
    A-933548
    Inhibitor
    A-933548 is a potent and selective inhibitor of calpain, with a Ki of 18 nM. A-933548 can be used for the research of Alzheimer's disease.
    A-933548
  • HY-100193
    FK-448 Free base
    Inhibitor
    FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM.
    FK-448 Free base
  • HY-156105
    8304-vs
    Inhibitor
    8304-vs is a macrocyclic anti-Plasmodial agent that covalently and irreversibly targets the Plasmodium proteasome. 8304-vs effectively inhibits the growth of Plasmodium falciparum.
    8304-vs
  • HY-135070
    Ac-RLR-AMC
    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.
    Ac-RLR-AMC
  • HY-108553
    Dihydroeponemycin
    Inhibitor
    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-P10003A
    iso-VQA-ACC TFA
    iso-VQA-ACC TFA is a constitutive proteasome substrate.
    iso-VQA-ACC TFA
  • HY-169135
    PROTAC 20S proteasome subunit β5 degrader 2
    Degrader
    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-P10007
    Z-Gly-Pro-Phe-Leu-CHO
    Inhibitor
    Z-Gly-Pro-Phe-Leu-CHO (Z-GPFL-CHO) is a tetrapeptide aldehyde that acts as a highly selective and potent proteasomal inhibitor (Ki = 1.5 µM for branched chain amino acid preferring, 2.3 µM for small neutral amino acid preferring, and 40.5 µM for chymotrypsin-like activities; IC50 = 3.1 µM for peptidyl-glutamyl peptide hydrolyzing activity).
    Z-Gly-Pro-Phe-Leu-CHO
  • HY-120035
    DD1
    Inhibitor 99.40%
    DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation.
    DD1
  • HY-P3356
    Cyclotheonellazole A
    Inhibitor
    Cyclotheonellazole A is a natural macrocyclic peptide and a potent elastase inhibitor (IC50=0.034 nM). Cyclotheonellazole A inhibits chymotrypsin with an IC50 value of 0.62 nM.
    Cyclotheonellazole A
  • HY-145542S
    Isovalerylcarnitine-d9 chloride
    Isovalerylcarnitine-d9 (chloride) is the deuterium labeled Isovalerylcarnitine (chloride)[1]. Isovalerylcarnitine chloride, a product of the catabolism of L-leucine, is a potent activator of the Ca2+-dependent proteinase (calpain) of human neutrophils[2].
    Isovalerylcarnitine-d<sub>9</sub> chloride
  • HY-P10003
    iso-VQA-ACC
    iso-VQA-ACC is a substrate for constitutive proteasome.
    iso-VQA-ACC
  • HY-P4291
    Z-Leu-Leu-Tyr-COCHO
    Inhibitor
    Z-Leu-Leu-Tyr-COCHO is a potent chymotrypsin-like activity inhibitor with a Ki value of 3.0 nM.
    Z-Leu-Leu-Tyr-COCHO
  • HY-125939
    Bortezomib-pinanediol
    Inhibitor
    Bortezomib-pinanediol is a proteasome inhibitor and a prodrug of Bortezomib (HY-10227). Bortezomib-pinanediol inhibits cell growth and can be used for study of multiple myeloma.
    Bortezomib-pinanediol
  • HY-P4348
    MeOSuc-Gly-Leu-Phe-AMC
    MeOSuc-Gly-Leu-Phe-AMC is a peptide substrate of proteasomal.
    MeOSuc-Gly-Leu-Phe-AMC
  • HY-117513
    CEP1612
    Inhibitor
    CEP1612 is a dipeptidyl proteasome inhibitor with the IC50 of 60 nM. CEP1612 induces p21(WAF1)and p27(KIP1) expression and cell apoptosis. CEP1612 shows anticancer activity in vivo.
    CEP1612
  • HY-P1259
    PR-39
    Inhibitor
    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-N2117R
    Isoginkgetin (Standard)
    Inhibitor
    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)
Cat. No. Product Name / Synonyms Application Reactivity