A potent anti-tumor agent used as a selective and irreversible inhibitor of the 20S proteasome; inhibits proteasome activity in cell growth assays (IC50 = 4 nM) and demonstrates potent cytotoxicity against B16-F10

Epoxomicin – 100 µg

Brand:
Cayman
CAS:
134381-21-8
Storage:
-20
UN-No:
Non-Hazardous - /

Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome. It inhibits proteasome activity in cell growth assays with an IC50 value of 4 nM and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells with IC50 values ranging from 2-44 nM.{13359,13358} By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10 nM.{13351} Intraperitoneal injection of 1.5 mg/kg epoxomicin given daily for two weeks induces Parkinson’s-like symptoms in rats and addition of 100 nM epoxomicin to rat ventral midbrain cultures results in apoptosis specific to dopaminergic neurons.{13355,16504} Epoxomicin-induced parkinsonism can be a useful model to examine mechanisms and therapies for the disease.  

 

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SKU: 10007806 - 100 µg Category:

Description

A potent anti-tumor agent used as a selective and irreversible inhibitor of the 20S proteasome; inhibits proteasome activity in cell growth assays (IC50 = 4 nM) and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells (IC50s = 2-44 nM)

Formal name: N-acetyl-N-methyl-L-isoleucyl-L-isoleucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-threoninamide

Synonyms:  BU 4061T

Molecular weight: 554.7

CAS: 134381-21-8

Purity: ≥98%

Formulation: A solution in DMSO

Product Type|Biochemicals|Natural Products|Microbial Metabolites||Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Cell Death||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Endocrinology & Metabolism|Bone Growth & Remodeling||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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