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Epoxomicin

Cat. No. M2193
Epoxomicin Structure
Synonym:

BU 4061T

Size Price Availability Quantity
1mg USD 137  USD137 In stock
5mg USD 400  USD400 In stock
10mg USD 700  USD700 In stock
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Quality Control
Biological Activity

Epoxomicin (BU 4061T) is a naturally occurring selective proteasome inhibitor with anti-inflammatory activity. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome. Epoxomicin (BU 4061T) 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. Epoxomicin also effectively inhibits NF-kappaB activation in vitro and potently blocks in vivo inflammation in the murine ear edema assay. In contrast to peptide aldehyde proteasome inhibitors, epoxomicin does not inhibit nonproteasomal proteases such trypsin, chymotrypsin, papain, calpain, and cathepsin B at concentrations of up to 50 microM. Treatment of proliferating cells with epoxomicin results in cell death through accumulation of ubiquinated proteins.

Product Citations
Customer Product Validations & Biological Datas
Source Mol Cell (2020), Figure 4, Epoxomicin (Abmole Bioscience Inc.)
Method Cell Culture
Cell Lines HeLa and HEK293T cell lines
Concentrations 100 µM
Incubation Time 2-12 hours
Results CCCP treatment induced accumulation of mitochondrion-localized fulllength PINK1 protein and an enhanced p-S222-TUFm signal;applying the proteasome inhibitor MG132 or epoxomicin elevated cytosolic and mitochondrial cleaved PINK1 and the p-S222-TUFm signal, and so did the autophagosome formation inhibitors CK636 and Baf-A1, but to a lesser extent
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 554.72
Formula C28H50N4O7
CAS Number 134381-21-8
Purity 98.57%
Solubility DMSO 10 mg/mL
Storage at -20°C
References

[1] Aboulaila M, et al. Vet Parasitol. Evaluation of the in vitro growth-inhibitory effect of epoxomicin on Babesia parasites.

[2] Czesny B, et al. Antimicrob Agents Chemother. The proteasome inhibitor epoxomicin has potent Plasmodium falciparum gametocytocidal activity.

[3] Schwarz K, et al. J Immunol. The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses.

[4] Meng L, et al. Proc Natl Acad Sci U S A. Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Epoxomicin, BU 4061T supplier, Proteasome, inhibitors

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