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T63321 |
20S Proteasome activator 1
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Proteasome
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20S Proteasome activator 1 is a 20S proteasome activator with IC50 of 0.3 μM for trypsin-like sites, 0.7 μM for chymotrypsin-like sites and 1.8 μM for caspase sites. 20S Proteasome activator 1 prevents the accumulation o... |
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T36218 |
19R(20S)-EpDPA
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19R(20S)-EpDPA is an oxylipin and a metabolite of docosahexaenoic acid .1,2It is formed from DHA by various cytochrome P450 (CYP) isoforms in a stereoselective manner.219R(20S)-EpDPA (30 nM) prevents calcium-induced incr... |
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T62255 |
20S Proteasome-IN-4
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20S Proteasome-IN-4 (Compound 7) is an orally active inhibitor of the 20S proteasome, selectively targeting the parasite form and demonstrating brain penetration capabilities. It exhibits a potent IC50 value of 6.3 nM ag... |
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T7814 |
Alloxan monohydrate
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Proteasome
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Alloxan Monohydrate is a glucose analog used to induce diabetes by destroying beta-cells. |
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T17011 |
TCH-165
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Proteasome
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TCH-165 is a small molecule modulator of proteasome assembly, resulting in an increase in 20S levels. The increase in the level of free 20S corresponds to enhanced proteolysis of IDPs. |
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T21854 |
Proteasome inhibitor IX
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PS-IX,AM114 |
Proteasome
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Proteasome inhibitor IX (PS-IX) is an inhibitor of chymotrypsin-like activity of the 20S proteasome (IC50 ~1 μM). Proteasome inhibitor IX shows potent anticancer activity. Proteasome inhibitor IX exhibits HCT116 p53+/+ c... |
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T2016 |
MLN9708
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Ixazomib Citrate |
Proteasome
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MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM/). The biologically active form of MLN9708 (Ixazomib Citrate) is MLN2238 in aqueous solutions or plasma. |
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T10061 |
(1S,2S)-Bortezomib
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Bortezomib |
Proteasome
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(1S,2S)-Bortezomib (Bortezomib) is an enantiomer of Bortezomib. Bortezomib is a reversible and selective inhibitor of the proteasome with a Ki of 0.6 nM for 20S proteasome. |
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T2399 |
Bortezomib
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Radiciol,NSC 681239,MG 341,DPBA,Brotezamide,LDP 341 |
Apoptosis
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NF-κB
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Proteasome
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Autophagy
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Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis. |
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T2122 |
Ixazomib
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MLN2238 |
Proteasome
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Caspase
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Autophagy
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Ixazomib (MLN2238) , a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also i... |
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T6041 |
Oprozomib
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PR-047,ONX 0912 |
Proteasome
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Autophagy
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Oprozomib (PR-047) (ONX 0912) , an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM)/LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has potential antineoplastic activity. |
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T1795 |
Carfilzomib
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PR-171 |
Apoptosis
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Proteasome
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Autophagy
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Carfilzomib (PR-171) is a proteasome inhibitor that irreversibly binds to the chymotrypsin of the 20S proteasome. Carfilzomib has antitumor activity and may be used to treat multiple myeloma. |
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T8397 |
Ixazomib citrate
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MLN9708 |
Proteasome
,
Autophagy
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Ixazomib citrate (MLN9708) is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (IC50 of 3.4 nM ) with potential antineoplastic activity. |
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T12579 |
RAMB4
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PTP1B-IN-9 |
Proteasome
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RAMB4 (PTP1B-IN-9) is a ubiquitin-proteasome system (UPS)-stressor,with anticancer activity. |
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T6300 |
Degrasyn
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WP1130 |
Apoptosis
,
JAK
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Bcr-Abl
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DUB
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Autophagy
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Degrasyn (WP1130) (WP1130), a specific deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor, also inhibits Bcr/Abl, which is a JAK2 transducer (without affecting 20S proteasome) and activator of transcri... |
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T36352 |
Suc-Leu-Tyr-AMC
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Suc-Leu-Tyr-AMC is a fluorescent substrate for calpain I and II and papain (another cysteine protease) that is used for measuring the chymotrypsin-like peptidase activity of the 20S proteasome (excitation max: 360 nm; em... |
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T21617 |
MG-115
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Z-LL-Nva-CHO |
Proteasome
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MG-115 (Z-LL-Nva-CHO) is a potent and reversible inhibitor of proteasome , with K i s of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteas... |
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T8464 |
RA-9
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Apoptosis
,
DUB
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RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs), with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines. |
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T37011 |
Boc-LRR-AMC
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Boc-LRR-AMC is a fluorogenic substrate for the trypsin-like activity of the 26S proteasome or 20S proteolytic core. Upon enzymatic cleavage by the 26S proteasome or 20S proteolytic core, amino-4-methylcoumarin (AMC) is r... |
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T27558 |
HT1042
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HT 1042,HT-1042 |
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HT1042 is an inhibitor of the β5i component of the 20S proteasome complex, it is used to aid in the treatment of inflammatory diseases, autoimmune and hematologic malignancies. |
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T37421 |
Ac-PAL-AMC
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Ac-PAL-AMC is a fluorogenic substrate for the β1i/LMP2 subunit of the 20S immunoproteasome. Upon cleavage, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify the activity of the β1i/L... |
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TP1308 |
Suc-Leu-Leu-Val-Tyr-AMC
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Suc-Leu-Leu-Val-Tyr-AMC is a fluorescent substrate for the 20S proteasome, other chymotrypsin-like proteases. |
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T82529 |
DPLG3
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DPLG3, a specific inhibitor of the chymotryptic-like β5i subunits, effectively inhibits mouse i-20S proteasomes with an IC50 value of 9.4 nM. This compound has applications in the research of immune diseases [1]. |
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T2154 |
MG-132
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Z-LLL-al,Z-Leu-Leu-Leu-CHO |
Apoptosis
,
Proteasome
,
Autophagy
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MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis. |
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T37420 |
Ac-ANW-AMC
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Ac-ANW-AMC,Ac-Ala-Asn-Trp-AMC |
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Ac-ANW-AMC is a fluorogenic substrate for the β5i/LMP7 subunit of the 20S immunoproteasome. [1] Upon cleavage, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify the activity of the β... |
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T78847 |
BC-05
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Others
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BC-05, an orally active inhibitor targeting CD13 and the proteasome, displays potent inhibition with IC50 values of 0.13 μM against human CD13 and 1.39 μM for the 20S proteasome. It is utilized in the research of multipl... |
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T73191 |
LONP1-IN-2
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LONP1-IN-2 is a potent, selective inhibitor of LONP1, demonstrating an IC50 value of 0.187 μM for LONP1 and over 10 μM for the 20S proteasome. This specificity underlines its potential utility in cancer research. |
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T74878 |
Enzyme-IN-1
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Enzyme-IN-1 (compound 1), a peptide-based inhibitor of N-terminal nucleophile (Ntn) hydrolases, specifically targets and inhibits the chymotrypsin-like activity (CT-L) of the 20S proteasome. This compound may possess pot... |
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T37417 |
Z-LLE-AMC
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Z-LLE-AMC is a fluorogenic substrate for the caspase-like post-glutamate peptide hydrolase of the 26S proteasome or 20S proteolytic core. Caspase-like activity can be quantified by fluorescent detection of free AMC (also... |
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T37418 |
Z-LLL-AMC
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Z-LLL-AMC is a fluorogenic substrate for the chymotrypsin-like activity of the 26S proteasome or 20S proteolytic core. Chymotrypsin-like activity can be quantified by fluorescent detection of free AMC (also known as 7-am... |
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T35773 |
Gliotoxin-13C13
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Gliotoxin-13C13 |
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Gliotoxin-13C13is intended for use as an internal standard for the quantification of gliotoxin by GC- or LC-MS. Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains ofAspergillusand other fungi with... |
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T36321 |
C6 Urea Ceramide
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C6 urea ceramide is an inhibitor of neutral ceramidase.1 It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and in HT-29 colon cancer cells but not in MEFs lacking neutral ceramidase. It i... |
