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Results for "

Proteasome activity

" in MedChemExpress (MCE) Product Catalog:

113

Inhibitors & Agonists

2

Screening Libraries

3

Fluorescent Dye

3

Biochemical Assay Reagents

21

Peptides

19

Natural
Products

3

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P2016
    Ac-Nle-Pro-Nle-Asp-AMC

    		Proteasome Others
    Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate for 26S proteasome. Ac-Nle-Pro-Nle-Asp-AMC can be used for the 26S proteasome caspase-like activity analysis .
    Ac-Nle-Pro-Nle-Asp-AMC
  • HY-P3414A
    Proteasome-activating peptide 1 TFA
    3 Publications Verification

    		 Proteasome Neurological Disease
    Proteasome-activating peptide 1 TFA is a peptide and a potent proteasome activator. Proteasome-activating peptide 1 TFA increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 TFA prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis .
    Proteasome-activating peptide 1 TFA
  • HY-107412
    Proteasome inhibitor IX

    PS-IX; AM114

    		 Proteasome Cancer
    Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity .
    Proteasome inhibitor IX
  • HY-134961
    Z-Ala-Arg-Arg-AMC

    Fluorogenic Proteasome Substrate; Z-ARR-AMC

    		 Proteasome Others
    Z-Ala-Arg-Arg-AMC (Fluorogenic Proteasome Substrate) is a fluorogenic substrate for assaying trypsin-like activity of proteasome .
    Z-Ala-Arg-Arg-AMC
  • HY-18741
    VR23
    1 Publications Verification

    		 Proteasome Apoptosis Metabolic Disease Cancer
    VR23 is a small molecule that potently inhibits the activities of trypsin-like proteasomes (IC50=1 nM), chymotrypsin-like proteasomes (IC50=50-100 nM), and caspase-like proteasomes (IC50=3 μM).
    VR23
  • HY-W054146
    RAMB4
    1 Publications Verification

    		 Proteasome Cancer
    RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity .
    RAMB4
  • HY-108552
    MG-115
    1 Publications Verification

    		 Proteasome Apoptosis Cancer
    MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis .
    MG-115
  • HY-P10317
    Suc-YVAD-AMC

    		Fluorescent Dye Others
    Suc-YVAD-AMC is used to measure the cysteine proteins of the proteasome.Suc-YVAD-AMC releases fluorescent AMC when cleaved by cysteine proteases to assess the enzymatic activity of the proteasome .
    Suc-YVAD-AMC
  • HY-144369
    Proteasome-IN-4

    		Proteasome Cancer
    Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research .
    Proteasome-IN-4
  • 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-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-158150
    20S Proteasome-IN-5

    		Proteasome Cancer
    20S Proteasome-IN-5 (Compound 5) is a macrocyclic inhibitor of the 20S Proteasome, with IC50 values of 0.19 and 52.5 μM for ChT-L and PGPH-L activity, respectively .
    20S Proteasome-IN-5
  • HY-115391
    Boc-LRR-AMC

    Boc-Leu-Arg-Arg-AMC

    		 Biochemical Assay Reagents Others
    Boc-LRR-AMC (Boc-Leu-Arg-Arg-AMC) is a fluorogenic substrate, which can be utilized for detecting the trypsin-like activity of the 26S proteasome or the 20S proteasome core .
    Boc-LRR-AMC
  • HY-10227
    Bortezomib
    180+ Cited Publications

    PS-341; LDP-341; NSC 681239

    		 Proteasome NF-κB Apoptosis Autophagy Cancer
    Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .
    Bortezomib
  • HY-W720448
    VR23-d8

    		Isotope-Labeled Compounds Proteasome Apoptosis Metabolic Disease
    VR23-d8 is the deuterium labeled VR23 (HY-18741). VR23 is a small molecule that potently inhibits the activities of trypsin-like proteasomes (IC50=1 nM), chymotrypsin-like proteasomes (IC50=50-100 nM), and caspase-like proteasomes (IC50=3 μM).
    VR23-d8
  • 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-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-10227S
    Bortezomib-d8

    PS-341-d8; LDP-341-d8; NSC 681239-d8

    		 Proteasome NF-κB Apoptosis Autophagy Cancer
    Bortezomib-d8 is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .
    Bortezomib-d8
  • HY-13067R
    Celastrol (Standard)

    Tripterine (Standard); Tripterin (Standard)

    		 Reference Standards Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite Inflammation/Immunology Cancer
    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-P3414
    Proteasome-activating peptide 1

    		Proteasome Neurological Disease
    Proteasome-activating peptide 1 is a peptide, which increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis .
    Proteasome-activating peptide 1
  • HY-P10060
    Boc-Val-Gly-Arg-AMC

    		Biochemical Assay Reagents Others
    Boc-Val-Gly-Arg-AMC is a peptide substrate that can be used to study activity of the proteasome .
    Boc-Val-Gly-Arg-AMC
  • HY-P4514
    Z-Gly-Gly-Arg-βNA

    		Proteasome Others
    Z-Gly-Gly-Arg-βNA is the synthetic peptide substrate of trypsin-like activities of the proteasome .
    Z-Gly-Gly-Arg-βNA
  • HY-10227R
    Bortezomib (Standard)

    PS-341 (Standard); LDP-341 (Standard); NSC 681239 (Standard)

    		 Reference Standards Proteasome NF-κB Apoptosis Autophagy Cancer
    Bortezomib (Standard) is the analytical standard of Bortezomib. This product is intended for research and analytical applications. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .
    Bortezomib (Standard)
  • HY-135070
    Ac-RLR-AMC

    Ac-Arg-Leu-Arg-AMC

    		 Proteasome Others
    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-135070B
    Ac-RLR-AMC TFA

    Ac-Arg-Leu-Arg-AMC TFA

    		 Proteasome Others
    Ac-RLR-AMC (Ac-Arg-Leu-Arg-AMC) TFA 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 TFA
  • HY-113824
    RID-F

    Ridaifen-F

    		 Proteasome Cancer
    RID-F (Ridaifen-F), a Tamoxifen (HY-13757A) derivative, is a nonpeptidic proteasome inhibitor. RID-F inhibits human 20S proteasome activity, with IC50s of 0.64, 0.34, and 0.43 μM for CT-L, T-L, and PGPH, respectively .
    RID-F
  • 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-129867
    Z-Leu-Leu-Leu-AMC

    Z-LLL-AMC

    		 Proteasome Others
    Z-Leu-Leu-Leu-AMC is a fluorogenic substrate for measuring the chymotrypsin-like protease activity of the 20S proteasome .
    Z-Leu-Leu-Leu-AMC
  • HY-W753820A
    Boc-LRR-AMC TFA

    Boc-Leu-Arg-Arg-AMC TFA

    		 Biochemical Assay Reagents Others
    Boc-LRR-AMC TFA (Boc-Leu-Arg-Arg-AMC TFA) is the TFA salt form of Boc-LRR-AMC (HY-115391). Boc-LRR-AMC TFA is a fluorogenic substrate, which can be utilized for detecting the trypsin-like activity of the 26S proteasome or the 20S proteasome core .
    Boc-LRR-AMC TFA
  • HY-13067
    Celastrol
    45+ Cited Publications

    Tripterine; Tripterin

    		 Proteasome Autophagy Mitophagy Apoptosis Endogenous Metabolite Antibiotic Bacterial Infection Inflammation/Immunology Cancer
    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. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
    Celastrol
  • HY-126874
    Tyropeptin A-4

    TP-101

    		 Proteasome Others
    Tyropeptin A-4 (TP-101) is a potent proteasome inhibitor with the ability to inhibit mammalian 20S proteasome activity. Tyropeptin A-4 exerts its inhibitory effect by binding to the site responsible for trypsin-like activity. Tyropeptin A-4 derivative TP-104 has a 20-fold increase in inhibitory activity over Tyropeptin A. TP-110 specifically inhibits trypsin-like activity without affecting PGPH and trypsin-like activity .
    Tyropeptin A-4
  • HY-P5280
    Ac-KQL-AMC

    		Ser/Thr Protease Others
    Ac-KQL-AMC is a fluorogenic substrate that can be used to quantify Trypsin-like activity, resulting in detectable fluorescence when cleaved by the proteasome .
    Ac-KQL-AMC
  • HY-W001023
    5-Amino-8-hydroxyquinoline

    5A8HQ

    		 Proteasome Cancer
    5-Amino-8-hydroxyquinoline (5A8HQ), a potential anticancer candidate, has promising proteasome inhibitory activity.
    5-Amino-8-hydroxyquinoline
  • HY-123053
    Z-Leu-Leu-Glu-AMC
    1 Publications Verification

    Z-LLE-AMC

    		 Proteasome Others
    Z-Leu-Leu-Glu-AMC is a substrate peptide, and can be used for determination of postacidic-like hydrolysing activity of 20S proteasome
    Z-Leu-Leu-Glu-AMC
  • HY-W273493
    4-Nitrochalcone

    2-(4-Nitrobenzylidene)acetophenone

    		 Proteasome Inflammation/Immunology
    4-Nitrochalcone (2-(4-Nitrobenzylidene)acetophenone) inhibits the proteasome, inhibits NF-κB activity induced by TNFα .
    4-Nitrochalcone
  • HY-13821
    Epoxomicin
    15+ 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-10227G
    Bortezomib

    PS-341; LDP-341; NSC 681239

    		 Proteasome NF-κB Apoptosis Autophagy Cancer
    Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .
    Bortezomib
  • HY-10985
    Marizomib
    10+ Cited Publications

    Salinosporamide A; NPI-0052

    		 Proteasome Cancer
    Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively) .
    Marizomib
  • HY-137286
    Z-Leu-Leu-Glu-βNA

    Z-Leu-Leu-Glu-β-naphthylamide

    		 Proteasome Others
    Z-Leu-Leu-Glu-βNA (Z-Leu-Leu-Glu-β-naphthylamide) is a substrate for determination of the glutamylpeptidyl-peptide hydrolase activity of the 20S proteasome .
    Z-Leu-Leu-Glu-βNA
  • HY-123052
    Ac-PAL-AMC

    		Proteasome Inflammation/Immunology
    Ac-PAL-AMC is a fluorogenic substrate specific for 20S proteasome LMP2/β1i activity .
    Ac-PAL-AMC
  • HY-163770
    Anticancer agent 233

    		Proteasome Cancer
    Anticancer agent 233 (compound 5g) is a 3,5-bis(arylmethylene)-4-piperidinone derivative with anticancer activity, with GI50 of 0.25 and 0.23 μM for cervical cancer (HeLa) and colon cancer (HCT116) cell lines, respectively. The chlorine atom on the aromatic ring of Anticancer agent 233 interacts well with the catalytic site of 20S proteasome, inhibiting the activity of 20S proteasome to exert its anticancer effect .
    Anticancer agent 233
  • HY-13259
    MG-132
    Maximum Cited Publications
    1443 Publications Verification

    Z-Leu-Leu-Leu-al

    		 Proteasome Autophagy Apoptosis Cancer
    MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis .
    MG-132
  • HY-158197
    RC-106

    		Sigma Receptor Proteasome Cancer
    RC-106 is a proteasome inhibitor (IC50: 35 μM) and Sigma receptor modulator with anticancer activity. RC-106 has antiproliferative activity against cancer cells including glioblastoma (GB) and multiple myeloma (MM) .
    RC-106
  • HY-117398
    HCI-2184

    		NEKs Cancer
    HCI-2184 is a Nek2 inhibitor with an IC50 of 39.90 nM. HCI-2184 significantly increases the effectiveness of Bortezomib (HY-10227) in inhibiting proteasome activity .
    HCI-2184
  • HY-10454
    Delanzomib
    2 Publications Verification

    CEP-18770

    		 Proteasome NF-κB Apoptosis Cancer
    Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities .
    Delanzomib
  • HY-136528
    RA-9

    		Deubiquitinase Apoptosis Cancer
    RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells .
    RA-9
  • HY-N2117
    Isoginkgetin
    15+ Cited Publications

    		 MMP Akt NF-κB Proteasome Apoptosis Autophagy Inflammation/Immunology Cancer
    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
  • 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-128903
    MC-Val-Cit-PAB-carfilzomib iodide

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-carfilzomib iodide is a agent-linker conjugate for ADC with potent antitumor activity by using carfilzomib (an irreversible proteasome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-carfilzomib iodide
  • HY-P4284
    Z-GGF-CMK

    		ClpP Proteasome Others
    Z-GGF-CMK is a protease inhibitor, inhibits ClpP1P2 and proteasome. Z-GGF-CMK exhibits cytotoxic activity against HepG2 cells with a CC50 value of 125 μM .
    Z-GGF-CMK

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