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

Proteasome

Proteasome

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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. 상품명 효과 Purity Chemical Structure
  • HY-112946
    LU-001i
    		Inhibitor
    LU-001i is a highly specific proteasome β1i (LMP2) inhibitor. LU-001i alone has no significant immunomodulatory effect, but when combined with the LMP7 inhibitor (PRN1126), it can exert anti-inflammatory and immunomodulatory effects. LU-001i can be used for the study of autoimmune diseases.
    LU-001i
  • HY-137897
    Bz-VGR-AMC
    		Substrate
    Bz-VGR-AMC is a substrate for the trypsin-like activity of the 20S proteasome. Bz-VGR-AMC can be used to measure the trypsin-like (β2) activity of the 20S proteasome.
    Bz-VGR-AMC
  • 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-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-18964G
    MG-101 (GMP)
    		Inhibitor
    MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer.
    MG-101 (GMP)
  • HY-P4514
    Z-Gly-Gly-Arg-βNA
    Z-Gly-Gly-Arg-βNA is the synthetic peptide substrate of trypsin-like activities of the proteasome.
    Z-Gly-Gly-Arg-βNA
  • HY-181524
    RA183-CO-C6-NHCO-NH-Boc
    		Ligand
    RA183-CO-C6-NHCO-NH-Boc is a proteasome ligand-linker conjugate that can be used for the synthesis of CAP-TAC (proteasome cap-targeted chimera), such as RAPRMT5 (HY-181521).
    RA183-CO-C6-NHCO-NH-Boc
  • 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-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-P11311
    NC-002
    		Inhibitor
    NC-002, a cell-permeable peptide, is a Trypsin-like proteasome inhibitor without inhibition of lysosomal cysteine proteases. NC-002 is the epoxyketone derivative of Leupeptin (HY-18234). NC-002 sensitizes myeloma cells to Bortezomib (HY-10227) and Carfilzomib (HY-10455). NC-002 can be used for cancers research.
    NC-002
  • 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-131350A
    LXE408 fumarate
    		Inhibitor
    LXE408 fumarate is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 fumarate has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 fumarate has a low propensity to cross the blood brain barrier. LXE408 fumarate has the potential for visceral leishmaniasis (VL) research.
    LXE408 fumarate
  • HY-145542S
    Isovalerylcarnitine-d9 chloride
    Isovalerylcarnitine-d9 chloride is the deuterium labeled Isovalerylcarnitine chloride (HY-145542). Isovalerylcarnitine chloride is a metabolite of leucine. Isovalerylcarnitine chloride can specifically activate calpain in human neutrophils. Isovalerylcarnitine chloride inhibits tumor cell proliferation and induces apoptosis. Elevated circulating levels of Isovalerylcarnitine chloride are negatively correlated with reduced lung cancer risk.
    Isovalerylcarnitine-d<sub>9</sub> chloride
  • HY-N16453
    (+)-Catechin 3-gallate
    		Inhibitor
    (+)-Catechin 3-gallate is an orally active polyphenolic compound that acts as a non-selective proteasome inhibitor. (+)-Catechin 3-gallate exerts antitumor effects by inducing apoptosis and suppressing inflammatory cytokines. (+)-Catechin 3-gallate is promising for research of cancers (e.g., breast, prostate) and neurodegenerative diseases (e.g., Alzheimer’s).
    (+)-Catechin 3-gallate
  • HY-180127
    UR238
    		Inhibitor
    UR238 is a proteasome inhibitor. UR238 reduces levels of the immunomodulator HE4. UR238 decreases PDL1 expression on cells. UR238 exhibits anticancer activity against epithelial ovarian cancer.
    UR238
Cat. No. 상품명 / Synonyms Application Reactivity