Epoxomicin A potent chymotrypsin-like proteasome inhibitor (CTRL)

Epoxomicin  (CAS 134381-21-8)

Epoxomicin | CAS 134381-21-8 is rated 5.0 out of 5 by 1.
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| See product citations (14)
Application: A potent chymotrypsin-like proteasome inhibitor (CTRL)
CAS Number: 134381-21-8
Purity: ≥95%
Molecular Weight: 554.7
Molecular Formula: C28H50N4O7
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ordering Information

Epoxomicin sc-201298 100 µg $205.00
Epoxomicin sc-201298A 250 µg $425.00

Epoxomicin is a potent proteasome inhibitor, primarily inhibiting the activity of CTRL(chymotrypsin-like proteasome). The novel α-epoxy ketone moiety of Epoxomicin forms covalent bonds with residues in particular catalytic subunits of the enzyme, disabling activity. The trypsin-like and peptidyl-glutamyl peptide hydrolyzing behavior of the proteasome were both inhibited by Epoxomicin as well (at 100 and 1,000-fold slower rates, respectively). Bone formation is heavily regulated by the ubiquitin-proteasome pathway, and Epoxomicin was shown to increase both bone volume and bone formation rates in rodents. Another study demonstrates that exposure to Epoxomicin and other proteasome inhibitors leads to dopaminergic cell death, producing a model of Parkinson's disease in vivo. Epoxomicin is an inhibitor of 20S Proteasome.


1. Hanada, M., et al. 1992. J. Antibiot. 45: 1746-1752. PMID: 1468981
2. Meng, L., et al. 1999. Proc. Natl. Acad. Sci. U.S.A. 96: 10403-10408. PMID: 10468620
3. Schwarz, K., et al. 2000. J. Immunol. 164: 6147-6157. PMID: 10843664
4. Princiotta, M.F., et al. 2001. Proc. Natl. Acad. Sci. U.S.A. 98: 513-518. PMID: 11149939
5. Garrett, I.R., et al. 2003. J. Clin. Invest. 111: 1771-1782. PMID: 12782679
6. McNaught, K.S., et al. 2004. Ann. Neurol. 56: 149-162. PMID: 15236415

Physical State :
Solubility :
Soluble in DMSO (10 mg/mL), and dichloromethane:methanol (9:1). Insoluble in water.
Storage :
Store at -20° C
Boiling Point :
~739.2° C at 760 mmHg (Predicted)
Density :
~1.1 g/cm3 (Predicted)
Refractive Index :
n20D 1.5
IC50 :
proteasome activity: IC50 = 4 nM; B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells: IC50 = 2-44 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
PubChem CID :
Merck Index :
14: 3630
MDL Number :

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Certificate of Analysis

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Epoxomicin Product Citations

See how others have used Epoxomicin. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 14 total

PMID: # 28667089
Molinski, SV. et al. 2017. Orkambi® and amplifier co-therapy improves function from a rare CFTR mutation in gene-edited cells and patient tissue. EMBO Mol Med.

PMID: # 25264277
Lupino, E. et al. 2014. Exposure of neuroblastoma cell lines to imatinib results in the upregulation of the CDK inhibitor p27(KIP1) as a consequence of c-Abl inhibition. Biochemical pharmacology. 92: 235-50.

PMID: # 24385906
Caffarelli, N. et al. 2013. Cyclin A degradation by primate cytomegalovirus protein pUL21a counters its innate restriction of virus replication. PLoS Pathog.. 9: e1003825.

PMID: # 23604491
Orre, M. et al. 2013. Reactive glia show increased immunoproteasome activity in Alzheimer's disease. Brain. 136: 1415-31.

PMID: # 24023882
Prasad, R. et al. 2013. Blocking Plasmodium falciparum development via dual inhibition of hemoglobin degradation and the ubiquitin proteasome system by MG132. PLoS ONE. 8: e73530.

PMID: # 22702336
Uyama, M. et al. 2012. Regulation of osteoblastic differentiation by the proteasome inhibitor bortezomib. Genes Cells. 17: 548-58.

PMID: # 18757370
Shi, W. et al. 2008. Disassembly of MDC1 foci is controlled by ubiquitin-proteasome-dependent degradation. J. Biol. Chem.. 283: 31608-31616.

PMID: # 16332688
Um, JW. et al. 2006. Parkin ubiquitinates and promotes the degradation of RanBP2. J. Biol. Chem.. 281: 3595-3603.

PMID: # 16687393
Chen, IY. et al. 2006. Histone H2A.z is essential for cardiac myocyte hypertrophy but opposed by silent information regulator 2alpha. J. Biol. Chem.. 281: 19369-19377.

PMID: # 15632159
Fioriti, L. et al. 2005. Cytosolic prion protein (PrP) is not toxic in N2a cells and primary neurons expressing pathogenic PrP mutations. J. Biol. Chem.. 280: 11320-11328.

Citations 1 to 10 of 14 total

How long will it remain stable in -20℃ DMSO?

Asked by: chemicalsmg
Thank you for your question. For epoxomicin, sc-201298, we do not recommend storing the aqueous solution for more than one day at -20℃.
Answered by: TechService7
Date published: 2017-01-03
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Rated 5 out of 5 by from Shi Shi, et. al. (PubMed ID 18757370) used epoxomicin in their proteosome inhibition studies on MCF-7 cells. -SCBT Publication Review
Date published: 2015-04-09
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