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Key inhibitor for use in proteasome research.
Cell permeable, potent and selective proteasome inhibitor originally isolated from Actinomycetes strain based on its potent in vivo antitumor activity. More potent inhibitor of the chymotrypsin-like activity of the proteasome than lactacystin (Prod. No. BML-PI104). Blocks also trypsin-like and PGPH activities of the proteasome. Regulates antigen presentation at non-toxic doses. Effectively inhibits NF-κB activation in vitro and potently blocks inflammation in vivo in the mouse ear edema assay.The ubiquitin-proteasome system (UPS) and autophagy serve as two complementary, reciprocally regulated protein degradation systems, thus blockade of UPS by Epoxomicin activates autophagy.
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Product Details
| Appearance |
Lyophilized. Very thin transparent film. |
|---|---|
| CAS |
134381-21-8 |
| Couple Target |
Proteasome |
| Couple Type |
Inhibitor |
| Formula |
C28H50N4O7 |
| MI |
14: 3630 |
| MW |
554.7 |
| Purity |
≥95% (HPLC) |
| Solubility |
Soluble in DMSO (15mg/ml) or dichloromethane:methanol (9:1); insoluble in water. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 3 months at -20°C. |
|---|---|
| Handling |
Protect from light. Avoid freeze/thaw cycles. |
| Long Term Storage |
-20°C |
| Shipping |
Blue Ice |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Proteasome activator 28γ (PA28γ) allosterically activates trypsin-like proteolysis by binding to the α-ring of the 20S proteasome: T.A. Thomas & D.M. Smith; J. Biol. Chem. 298, 102140 (2022), Abstract
- Archaeal Connectase is a specific and efficient protein ligase related to proteasome β subunits: A.C.D. Fuchs, et al.; PNAS 118, 2017871118 (2021), Abstract
- Early-onset impairment of the ubiquitin-proteasome system in dopaminergic neurons caused by α-synuclein: C. McKinnon, et al.; Acta Neuropathol. Commun. 8, 17 (2020), Abstract — Full Text
- miR-34a is upregulated in AIP-mutated somatotropinomas and promotes octreotide resistance: Bogner, E. M., Daly, A. F., et al.; Int. J. Cancer 147, 3523 (2020), Abstract
- Synaptogenesis Stimulates a Proteasome-Mediated Ribosome Reduction in Axons: Costa, R. O., Martins, H., et al.; Cell Rep. 28, 864 (2019), Abstract
- HIV Controllers Exhibit Effective CD8+ T Cell Recognition of HIV-1-Infected Non-activated CD4+ T Cells: Monel, B., McKeon, A., et al.; Cell Rep. 27, 142 (2019), Abstract
- A novel probe to assess cytosolic entry of exogenous proteins: Lu, Q., Grotzke, J. E., et al.; Nat. Commun. 9, 3104 (2018), Abstract
- Nogo-A interacts with TrkA to alter nerve growth factor signaling in Nogo-A-overexpressing PC12 cells: R.G. Farrer, et al.; Cell. Signal. 44, 20 (2018), Abstract
- Bassoon Controls Presynaptic Autophagy through Atg5: Okerlund, N. D., Schneider, K., et al.; Neuron 93, 897 (2017), Abstract
- Caspase vinyl sulfone small molecule inhibitors prevent axonal degeneration in human neurons and reverse cognitive impairment in Caspase-6-overexpressing mice: P. Pakavathjkumar, et al.; Mol. Neurodegener. 12, 22 (2017), Abstract — Full Text
- Proteasome activity regulates CD8+ T lymphocyte metabolism and fate specification: Widjaja, C. E., Olvera, J. G., et al.; J. Clin. Invest. 127, 3609 (2017), Abstract
- The inhibition of IGF-1 signaling promotes proteostasis by enhancing protein aggregation and deposition: Moll, L., Ben-Gedalya, T., et al.; FASEB J. 30, 1656 (2016), Abstract
- A small-molecule Nrf1 and Nrf2 activator mitigates polyglutamine toxicity in spinal and bulbar muscular atrophy: Bott, L. C., Badders, N. M., et al.; Hum. Mol. Genet. 25, 1979 (2016), Abstract
- Diagnostic and clinical relevance of the autophago-lysosomal network in human gliomas: Jennewein, L., Ronellenfitsch, M. W., et al.; Oncotarget 7, 20016 (2016), Abstract
- Downregulation of 26S proteasome catalytic activity promotes epithelial-mesenchymal transition: Banno, A., Garcia, D. A., et al.; Oncotarget 7, 21527 (2016), Abstract
- Comparative Proteomics Reveals Strain-Specific β-TrCP Degradation via Rotavirus NSP1 Hijacking a Host Cullin-3-Rbx1 Complex: S. Ding, et al.; PLoS Pathology 12, e1005929 (2016), Application(s): Cell treatment, Abstract — Full Text
- Prion-mediated neurodegeneration is associated with early impairment of the ubiquitin-proteasome system: C. McKinnon, et al.; Acta Neuropathol. 131, 411 (2016), Application(s): Determined background activity caused by non-proteasomal degradation, Abstract — Full Text
- Methylene Blue Inhibits Caspases by Oxidation of the Catalytic Cysteine: Pakavathkumar, P., Sharma, G., et al.; Sci. Rep. 5, 13730 (2015), Abstract
- Modified vaccinia virus Ankara-infected dendritic cells present CD4+ T-cell epitopes by endogenous major histocompatibility complex class II presentation pathways: Thiele, F., Tao, S., et al.; J. Virol. 89, 2698 (2015), Abstract
- Proteasome inhibition slightly improves cardiac function in mice with hypertrophic cardiomyopathy: Schlossarek, S., Singh, S. R., et al.; Front. Physiol. 5, 484 (2015), Abstract
- The regulation of glucose on milk fat synthesis is mediated by the ubiquitin-proteasome system in bovine mammary epithelial cells: L. Liu, et al.; Biochem. Biophys. Res. Commun. 465, 59 (2015), Application(s): Cell culture, Abstract
- Bortezomib Amplifies Effect on Intracellular Proteasomes by Changing Proteasome Structure: D.S. Pitcher, et al.; EBioMedicine 2, 642 (2015), Application(s): Western Blot, Abstract
- Superior antimitogenic and chemosensitization activities of the combination treatment of the histone deacetylase inhibitor apicidin and proteasome inhibitors on human colorectal cancer cells: Abaza, M. S., Bahman, A. M., et al.; Int. J. Oncol. 44, 105 (2014), Abstract
- The small heat shock protein B8 (HSPB8) confers resistance to bortezomib by promoting autophagic removal of misfolded proteins in multiple myeloma cells: M. Hamouda, et al.; Oncotarget 5, 6252 (2014), Application(s): Analysis of velcade resistant multiple myeloma human cells by WB, Assay, Abstract — Full Text
- Removal of damaged proteins during ES cell fate specification requires the proteasome activator PA28: M. Hernebring, et al.; Sci. Rep. 3, 1381 (2013), Abstract — Full Text
- Agonist-induced down-regulation of endogenous protein kinase c α through an endolysosomal mechanism: Lum, M. A., Pundt, K. E., et al.; J. Biol. Chem. 288, 13093 (2013), Abstract
- Role of cell-type-specific endoplasmic reticulum-associated degradation in polyomavirus trafficking: Bennett, S. M., Jiang, M., et al.; J. Virol. 87, 8843 (2013), Abstract
- Pathogen signatures activate a ubiquitination pathway that modulates the function of the metabolic checkpoint kinase mTOR: S. Ivanov & C. Roy; Nat. Immunol. 14, 1219 (2013), Application(s): Analysis of mouse macrophages by WB, PCR, Abstract — Full Text
- Processing of recombinant Listeria monocytogenes proteins for MHC class I presentation follows a dedicated, high-efficiency pathway: Wolf, B. J., Princiotta, M. F., et al.; J. Immunol. 190, 2501 (2013), Abstract
- Protein carbonylation and aggregation precede neuronal apoptosis induced by partial glutathione depletion: A. Dasgupta, et al.; ASN Neuro 4, e00084 (2012), Abstract — Full Text
- Novel Cell- and Tissue-Based Assays for Detecting Misfolded and Aggregated Protein Accumulation Within Aggresomes and Inclusion Bodies: D. Shen, et al.; Cell Biochem. Biophys. 60, 173 (2011), Abstract — Full Text
- Role of autophagy and proteasome degradation pathways in apoptosis of PC12 cells overexpressing human alpha-synuclein: F. Yang, et al.; Neurosci. Lett. 454, 203 (2009), Abstract
- Establishment and some characteristics of epoxomicin (a proteasome inhibitor) resistant variants of the human squamous cell carcinoma cell line, A431: K. Ohkawa, et al.; Int. J. Oncol. 24, 425 (2004), Abstract
- The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses: K. Schwarz, et al.; J. Immunol. 164, 6147 (2000), Abstract
- Total synthesis of the potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology: N. Sin, et al.; Bioorg. Med. Chem. Lett. 9, 2283 (1999), Abstract
- Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency: K.B. Kim, et al.; Bioorg. Med. Chem. Lett. 9, 3335 (1999), Abstract
- Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity: L. Meng, et al.; PNAS 96, 10403 (1999), Abstract
- Epoxomicin, a new antitumor agent of microbial origin: M. Hanada, et al.; J. Antibiot. (Tokyo) 45, 1746 (1992), Abstract
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