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Results for "

Proteasome inhibition

" in MedChemExpress (MCE) Product Catalog:

30

Inhibitors & Agonists

6

Peptides

2

Inhibitory Antibodies

5

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Targets Recommended:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-P9915
    Daratumumab
    10+ Cited Publications

    Anti-Human CD38, Human Antibody; HuMax-CD38; JNJ-54767414

    		 CD38 ADC Antibody Inflammation/Immunology Cancer
    Daratumumab (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab has anti-multiple myeloma (MM) effect. Daratumumab impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
    Daratumumab
  • HY-159607
    PRT3789

    		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-P9915A
    Daratumumab (Anti-CD38)
    10+ Cited Publications

    Anti-Human CD38, Human Antibody (PBS)

    		 ADC Antibody CD38 Cancer
    Daratumumab (PBS) (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab (PBS) has anti-multiple myeloma (MM) effect. Daratumumab (PBS) impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
    Daratumumab (Anti-CD38)
  • HY-N7056
    4'-Hydroxychalcone
    3 Publications Verification

    		 Oxidative Phosphorylation Proteasome Inflammation/Immunology Cancer
    4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria .
    4'-Hydroxychalcone
  • HY-19934
    Pifusertib

    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-19934A
    Pifusertib hydrochloride

    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-P2483B
    Octaarginine acetate

    		Bacterial Proteasome Infection Inflammation/Immunology Cancer
    Octaarginine acetate is a cell-penetrating peptide and proteasome inhibitor. Octaarginine acetate exhibits mixed-type inhibition against 20S proteasome chymotrypsin-like, caspase-like, and trypsin-like activities, and inhibits 26S proteasome activity with decreased efficiency. Octaarginine acetate induces ubiquitin-conjugated protein accumulation, mediates HSPG-dependent cellular internalization via macropinocytosis, enhances liposomal cargo uptake and gene delivery. Octaarginine acetate can be used for the research of cervix carcinoma, collagen antibody-induced arthritis, and bacterial infections .
    Octaarginine acetate
  • HY-P2483
    Octaarginine

    		Proteasome Bacterial Infection Inflammation/Immunology Cancer
    Octaarginine is a cell-penetrating peptide and proteasome inhibitor. Octaarginine exhibits mixed-type inhibition against 20S proteasome chymotrypsin-like, caspase-like, and trypsin-like activities, and inhibits 26S proteasome activity with decreased efficiency. Octaarginine induces ubiquitin-conjugated protein accumulation, mediates HSPG-dependent cellular internalization via macropinocytosis, enhances liposomal cargo uptake and gene delivery. Octaarginine can be used for the research of cervix carcinoma, collagen antibody-induced arthritis, and bacterial infections .
    Octaarginine
  • HY-119288
    BC-23

    NSC 45382

    		 Proteasome Cancer
    BC-23 (NSC 45382) is a proteasome inhibitor. BC-23 exhibits good inhibition of CT-L activity of the proteasome and is selective for malignant over normal cells .
    BC-23
  • HY-P11331
    Az-NC-002

    		Proteasome Others
    Az-NC-002 is a Proteasome trypsin-like site (β2) and immunoproteasome β2i-specific active probe. Az-NC-002 has weak off-target effects with no significant inhibition for Cathepsin D (HY-P2750), but this inhibition reacts outside of the active site or influence on a small fraction of the enzyme .
    Az-NC-002
  • HY-161180
    Antitumor agent-136

    		NAMPT Cancer
    Antitumor Agent-136 (Compound 17) is a potent broad-spectrum antitumor agent and a NAMPT inhibitor with an IC50 of 9.5 nM. Antitumor Agent-136 can reduce the levels of intracellular and extracellular NAMPT protein through the ubiquitin proteasome pathway, thus achieving tumor inhibition .
    Antitumor agent-136
  • HY-137281
    HMB-Val-Ser-Leu-VE

    		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-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-164689
    Cadmium pyrithione

    		Proteasome Cancer
    Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models .
    Cadmium pyrithione
  • HY-N13904
    Argyrin A

    		Proteasome Cancer
    Argyrin A, a cyclical peptide, is a potent antitumoral agent. Argyrin A exerts its effects through a potent inhibition of the proteasome. Argyrin A leads to increased endogenous p27 kip1 levels by preventing protein turnover .
    Argyrin A
  • HY-P2483A
    Octaarginine TFA

    		Proteasome Bacterial Infection Neurological Disease Cancer
    Octaarginine TFA is a cell-penetrating peptide and proteasome inhibitor. Octaarginine TFA exhibits mixed-type inhibition against 20S proteasome chymotrypsin-like, caspase-like, and trypsin-like activities, and inhibits 26S proteasome activity with decreased efficiency. Octaarginine TFA induces ubiquitin-conjugated protein accumulation, mediates HSPG-dependent cellular internalization via macropinocytosis, enhances liposomal cargo uptake and gene delivery. Octaarginine TFA can be used for the research of cervix carcinoma, collagen antibody-induced arthritis, and bacterial infections .
    Octaarginine TFA
  • HY-141543
    YW2065

    		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-N13917
    Argyrin B

    		Proteasome Bacterial Infection Cancer
    Argyrin B, a natural product cyclic peptide, is a reversible, non-competitive immunoproteasome inhibitor. Argyrin B shows selective inhibition of the β5i and β1i sites of the immunoproteasome over the β5c and β1c sites of the constitutive proteasome with nearly 20-fold selective inhibition of β1i over the homologous β1c. Argyrin B has antibacterial effects .
    Argyrin B
  • HY-P11311
    NC-002

    		Proteasome Cancer
    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-138958
    HT1171

    		Bacterial Virus Protease Infection
    HT1171 is a potent and selective inhibitor of mycobacterium tuberculosis proteasome. HT1171 shows strong anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv with an MIC90 of 2 μg/mL and an MIC of 4 μg/mL. When HT1171 concentration is 100 μM, the inhibition rate of human normal hepatocytes L02 is 53.8%. HT1171 can be used in the research of antitubercular agent .
    HT1171
  • HY-N7890
    Isomoreollic acid

    		Proteasome Cancer
    Isomoreollic acid is a cage xanthonoid. Isomoreollic acid exhibits cytotoxicity against colon cancer cells, with an IC50 > 10 μM for proteasome inhibition. Isomoreollic acid is present in the stem bark of Garcinia lateriflora. Isomoreollic acid can be used in colon cancer research .
    Isomoreollic acid
  • HY-N7056R
    4'-Hydroxychalcone (Standard)

    		Reference Standards Proteasome Oxidative Phosphorylation Inflammation/Immunology Cancer
    4'-Hydroxychalcone (Standard) is the analytical standard of 4'-Hydroxychalcone (HY-N7056). This product is intended for research and analytical applications. 4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria .
    4'-Hydroxychalcone (Standard)
  • HY-182760
    MN33-63

    		DNA Alkylator/Crosslinker Bcl-2 Family Caspase Apoptosis Topoisomerase Cancer
    MN33-63 is a Bcl-2 inhibitor, caspase-3 activator and DNA crosslinker with broad-spectrum anticancer activity. MN33-63 improves the water solubility of SN-38 (HY-13704), inhibits tumor growth and proliferation in a dose-dependent manner, and causes no obvious toxicity. MN33-63 relieves the inhibition of the mitochondrial apoptotic pathway, initiates the apoptosis program, inhibits Topo I activity, and promotes its degradation via the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-63 induces DNA crosslinking, G2/M cell cycle arrest, inhibition of cancer cell migration, and cancer cell apoptosis through the mitochondrial pathway. MN33-63 can be used in the research of colorectal cancer, cervical cancer, hepatocellular carcinoma, lung adenocarcinoma and gastric cancer .
    MN33-63
  • HY-182800
    IBA-11

    		Molecular Glues Casein Kinase Cancer
    IBA-11 is a selective CRBN-dependented CK1α molecular glue degrader. IBA-11 binds to the canonical tri-tryptophan pocket of CRBN, forming a ternary complex with CK1α to mediate its degradation. IBA-11 induces CRBN-dependent ubiquitin-proteasome system-mediated degradation of CK1α. IBA-11 exhibits cytotoxicity against cancer cells. IBA-11 demonstrates in vitro metabolic stability in rat liver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia .
    IBA-11
  • HY-181967
    PROTAC PARP1 degrader-5

    		PROTACs PARP DNA/RNA Synthesis PD-1/PD-L1 Cancer
    PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC50 of 0.12 μM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma .
    PROTAC PARP1 degrader-5
  • HY-180970
    TD-004

    		PROTACs Anaplastic lymphoma kinase (ALK) Cancer
    TD-004 is a potent ALK PROTAC degrader. TD-004 exhibits anti-ALK inhibitory activity with an IC50 of 0.11 µM and selectively inhibits the proliferation of SU-DHL-1 and H3122 cells (ALK-positive cancer cells) with IC50s of 0.058 µM and 0.28 µM, respectively. TD-004 induces degradation of ALK fusion proteins (NPM-ALK and EML4-ALK) via recruitment of the VHL E3 ligase and the proteasome pathway. TD-004 demonstrates significant tumor growth inhibition with a favorable safety profile in vivo. TD-004 can be used for the research of anaplastic large cell lymphoma and non-small cell lung cancer .
    TD-004
  • HY-182759
    MN33-47

    		DNA Alkylator/Crosslinker Topoisomerase Caspase Bcl-2 Family Apoptosis Cancer
    MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer .
    MN33-47
  • HY-181758
    PROTAC CBP/p300/BRD4 Degrader-1

    		PROTACs Epigenetic Reader Domain Histone Acetyltransferase c-Myc Apoptosis Cancer
    PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer .
    PROTAC CBP/p300/BRD4 Degrader-1
  • HY-179499
    PROTAC EZH2 Degrader-9

    		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
  • HY-181907
    NBE5

    		HyT Keap1-Nrf2 HSP Inflammation/Immunology
    NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C) .
    NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).
    NBE5

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