Catalog No.
Product Name
Application
Product Information
Citations
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20S Proteasome Inhibitor
Cerpegin is a potent inhibitor of the 20S proteasome, which plays a critical role in the degradation of ubiquitinated proteins. This compound exhibits significant biological activities including anti-inflammatory, analgesic, and antiulcer effects, making it a valuable tool in research focused on proteasome-related pathways and therapeutic applications. Its mechanism of action allows for exploration in models of neuroprotection and various inflammatory conditions. -
Proteasome Inhibitor
Phepropeptin D is a microbial secondary metabolite that functions as a proteasome inhibitor, exhibiting an IC50 of 7.8 μg/mL. This compound plays a significant role in the regulation of protein degradation pathways, making it valuable for studies related to cellular proteostasis and cancer research. Its ability to modulate proteasome activity positions Phepropeptin D as a useful tool for investigating therapeutic strategies targeting proteasome-mediated pathways. -
Proteasome Control
Bortezomib impurity A is a metabolite of the 20S proteasome inhibitor Bortezomib, functioning as a key control for proteasome activity. This compound is useful in research applications focused on the mechanisms of proteasome inhibition and related signaling pathways. Its characterization aids in the development and quality assessment of proteasome-targeted therapeutics. -
HER2 Inhibitor
JBJ-08-178-01 is a selective tyrosine kinase inhibitor targeting mutant forms of the human epidermal growth factor receptor 2 (HER2). It demonstrates significant antitumor activity by reducing both the kinase activity and protein levels of HER2 through the induction of proteasomal degradation. This compound holds potential for research applications in non-small-cell lung cancer, providing insights into therapeutic mechanisms against HER2-driven malignancies. -
Proteasome Inhibitor
4-Nitrochalcone serves as a proteasome inhibitor, specifically targeting the proteasomal degradation pathway. It effectively inhibits the activity of NF-κB induced by TNFα, making it a valuable tool for studying inflammatory processes and signaling pathways. This compound is utilized in research focused on cancer, neurodegenerative diseases, and other conditions where proteasome activity plays a critical role. -
Antitumoral Agent
Argyrin A is a cyclical peptide that functions as a potent antitumoral agent through its ability to inhibit the proteasome. This inhibition results in increased levels of endogenous p27kip1 by blocking protein turnover, thereby contributing to its antitumor activity. Argyrin A is valuable for research applications focusing on cancer biology and therapeutic development targeting proteasomal pathways. -
Proteasome Inhibitor
Phepropeptin A is a microbial secondary metabolite that functions as a potent proteasome inhibitor, exhibiting an IC50 of 21 μg/mL. This compound is valuable for research applications focusing on the regulation of protein degradation pathways. Phepropeptin A can be utilized in studies aimed at understanding the role of proteasomal inhibition in cellular processes and disease models, particularly in cancer research and neurodegenerative disorders. -
Proteasome Inhibitor
Phepropeptin C is a proteasome inhibitor with a reported IC50 of 12.5 μg/mL. This microbial secondary metabolite disrupts protein degradation pathways, leading to the accumulation of regulatory proteins and altered cellular responses. Its ability to modulate proteasome activity makes it a valuable tool for research into cancer biology and other diseases characterized by dysregulated protein homeostasis. -
Chymase Inhibitor
BI-1942 is a potent chymase inhibitor with an IC50 of 0.4 nM for human chymase. This chemical probe is primarily utilized in research related to ophthalmic diseases, enabling the exploration of chymase's role in ocular pathologies. Its selective inhibition provides a valuable tool for investigating the therapeutic potential in conditions where chymase is implicated. -
Proteasome Inhibitor
RID-F (Ridaifen-F) is a nonpeptidic proteasome inhibitor that targets the human 20S proteasome. It demonstrates significant inhibitory activity with IC50 values of 0.64 µM for caspase-like (CT-L), 0.34 µM for trypsin-like (T-L), and 0.43 µM for post-glutamyl (PGPH) activities. RID-F is utilized in research focused on cellular degradation pathways, cancer biology, and therapeutic approaches targeting proteasome dysfunction. -
Proteasome Inhibitor
Chymase-IN-2 is a potent proteasome inhibitor that selectively modulates chymase activity. It exhibits significant efficacy in addressing inflammatory responses and disorders associated with serine protease activity. This compound is valuable for research aimed at understanding protease-mediated pathways and their implications in various diseases. -
Proteasome Inhibitor
Neurodegenerative Disorder-Targeting Compound 1 is a proteasome inhibitor that selectively targets calpain activity. This compound is designed to modulate cellular protein turnover, making it a valuable tool for studying the mechanisms of neurodegeneration. Its application spans various research areas, including the investigation of proteolytic pathways in neurodegenerative disorders and the exploration of therapeutic interventions aimed at enhancing neuronal survival. -
Proteasome inhibitor
CEP-18770 is a novel orally active proteasome inhibitor with a favorable tumor selectivity profile for the treatment of MM and other malignancies responsive to proteasome inhibition. -
NF-kB inhibitor/Proteasome activator
18α-Glycyrrhetinic acid (18α-GA) is a bioactive triterpenoid found in licorice. It shows selective inhibition of 11-HSD1 (11-hydroxysteroid dehydrogenase 1). -
proteasome inhibitor
Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1. -
Proteasome inhibitor
ONX 0912 is a tripeptide epoxyketone, which inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies. -
20S proteasome inhibitor
Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM. -
proteasome inhibitor
(R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132. -
chymotrypsin inhibitor
FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM. -
proteasome subunit Rpn11 inhibitor
Rpn11-IN-1 (Capzimin intermediate) is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM. -
alpains 1 and 2 inhibitor
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD). -
20S proteasome inhibitor
Aclarubicin A, an anthracycline drug, specific inhibitor of the 20S proteasome chymotrypsin-like activity. -
20S proteasome inhibitor
AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 uM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins. -
Proteasome inhibitor
Dihydroeponemycin is an inhibitor of proteasome and antitumor reagent. -
20S proteasome inhibitor
Clasto-lactacystin b-lactone was later identified as the active metabolite of lactacystin, resulting from the elimination of cysteine and the formation of a reactive b-lactone. -
LonP1/ CT-L proteasome inhibitor
BT317 is a selective inhibitor of mitochondrial Lon peptidase I (LonP1) and the caspase-like (CT-L) activity of the proteasome. This compound has been shown to increase the production of reactive oxygen species (ROS), leading to apoptosis in astrocytoma cells. BT317 exhibits significant antitumor activity, making it a valuable reagent for research in cancer biology and therapeutic applications targeting gliomas. -
Proteasome Inhibitor
YSY01A is a potent proteasome inhibitor that promotes apoptosis in cancer cells, demonstrating IC50 values of 51.0 nM in HEK293T, 9.2 nM in A549, 5.2 nM in MCF-7, 8.9 nM in MGC-803, and 35.4 nM in PC-3M cell lines. This compound effectively disrupts constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A serves as a valuable tool for research in cancer therapy and apoptosis mechanisms. -
20S proteasome Inhibitor
BSc2118 is a potent inhibitor of the 20S proteasome, exhibiting an IC50 of approximately 50 nM. This compound induces G2/M phase cell cycle arrest and apoptosis in myeloma cells while inhibiting cytoprotective autophagy and tumor angiogenesis. Additionally, BSc2118 reduces matrix metalloproteinase 9 (MMP9) activity, promotes angioneurogenesis, and mitigates cerebral toxicity associated with recombinant tissue-type plasminogen activator. Its applications are relevant in the studies of cerebral ischemia and multiple myeloma. -
Proteasome Inhibitor
CEP1612 is a dipeptidyl proteasome inhibitor that exhibits an IC50 of 60 nM. This compound induces the expression of cell cycle regulators p21(WAF1) and p27(KIP1), leading to enhanced apoptotic activity in cancer cells. Due to its ability to disrupt proteasomal degradation, CEP1612 demonstrates significant anticancer efficacy in vivo, making it a valuable tool for research into cancer therapeutics. -
Proteasome Inhibitor
NIC-0102 is an orally active proteasome inhibitor that specifically targets NLRP3 inflammatory vesicle activation, exhibiting a pIC50 of 7.55. This compound demonstrates significant anti-inflammatory effects in models of dextran sulfate sodium (DSS)-induced ulcerative colitis. Additionally, NIC-0102 is effective in inhibiting the production of pro-IL-1β, making it a valuable tool for research in inflammation and related pathways. -
Proteasome Inhibitor
UR238 is a potent proteasome inhibitor that decreases the levels of the immunomodulatory protein HE4. Additionally, UR238 effectively reduces PDL1 expression on various cell types. Its anticancer properties make it a valuable reagent for research focusing on epithelial ovarian cancer.
