Epoxomicin

Catalog No.S7038 Synonyms: BU-4061T,Aids010837

Epoxomicin Chemical Structure

Molecular Weight(MW): 554.72

Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate.

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Cited by 4 Publications

2 Customer Reviews

  • Epoxomicin did not inhibit the EV71-induced PMLIII and IV degradation. Cell lysates were prepared from 293T cells infected or mock-infected with EV71 at a multiplicity of infection (MOI) of 5 for 24 or 48 h in the presence or absence of epoxomicin (1 µM). At 24 h post-infection (p.i.) (left panels) or 48 h p.i. (right panels), 60 μg of protein extracted from each treatment were separated on SDS-PAGE and analyzed by performing a Western blot analysis using antibodies specific for PMLIII and IV (top panels), VP1 (middle panels), and GAPDH, which served as an internal loading control (bottom panels). PMLIII and IV were quantified by performing densitometry and are presented relative to the mock infection, which was set as 1.0. VP1 was quantified and is presented relative to that in the EV71-infected 293T cells at 24 h p.i. (left panels) or 48 h p.i. (right panels). The density value of VP1 without epoxomicin is set as 1.0. The experiment was performed three times, and representative results are shown.

    Front Immunol, 2018, 9:1268. Epoxomicin purchased from Selleck.

    Immature monocyte-derived dendritic cells (moDCs) were incubated 30 min prior and during the 3 h antigen (gp100/AZN-D1) pulse with 0.1% DMSO (vehicle), chloroquine (25 µM), MG132 (10 µM), epoxomicin (0.25 µM), and cathepsin S inhibitor (5 µM). Groups are significantly different compared to AZN-D1.

    Front Immunol, 2018, 9:1231. Epoxomicin purchased from Selleck.

Purity & Quality Control

Choose Selective Proteasome Inhibitors

Biological Activity

Description Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate.
Features Epoxomicin is a natural product isolated from an Actinomycetes species.
Targets
20S proteasome [1]
In vitro

Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome. Epoxomicin (100 nM) results in a 30-fold increase in the levels of p53 protein, a known target of the proteasome, in HUVECs. Epoxomicin (10 μM) results in the accumulation of ubiquitinated proteins in HeLa cells. Epoxomicin (10 μM) inhibits IκBα degradation by 10-fold in HeLa cells. Epoxomicin (10 μM) produces a significant dose-dependent reduction in TNF-α-stimulated NF-κB DNA-binding activity in HeLa cells. [1] Epoxomicin inhibits proliferating of EL4 lymphoma cells with biotinylated chimerae with IC50 of 4 nM. [2] Epoxomicin (1 μM) leads to a reduction of LCMV GP33 presentation and an enhancement of GP276 presentation. [3] Epoxomicin inhibits growth of Babesia bigemina with IC50 of 4 nM. Epoxomicin (0.5 mg/kg and 0.05 mg/kg) results in peak parasitemia levels of 34.8% and 42.3% in B. microti. [4] Epoxomicin (100 nM) decreases the total parasitemia by 78%, 86% and 77% in Plasmodium falciparum. Epoxomicin (10 μM) inhibits gametogenesis and exflagellation as well as development into oocysts of anopheles mosquitoes. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC3 cell NV6yPXJLWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxtKGyrbnWsJGlEPTB;MD6wNFEh|ryP MV2xOlY5PjV|Nx?=
WM266.4 cells M4juZ2N6fG:2b4jpZ4l1gSCjc4PhfS=> MojNO|IhcA>? NGi3SWtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBYVTJ4Nj60JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCDVGDsbZRmKGG|c3H5MEBKSzVyPUCuNFA1QCEQvF2= M2e0UFIzOjB4OE[5
human LCL cells M4rKR2Z2dmO2aX;uJIF{e2G7 MlfFNVIhcA>? MWXJcohq[mm2aX;uJI9nKGOqeX3veJJ6eHOrbj3sbYtmKGGldHn2bZR6KG:oIEKwV{Bxem:2ZXHzc41mKGKndHGyJIlvKGi3bXHuJGxEVCClZXzsd{Bi\nSncjCxNkBpenNuIFnDOVA:OC5yMEWg{txO M4DofFIxPjh5NkC5
human DLD1 cells M4PTW2Z2dmO2aX;uJIF{e2G7 MYDJcohq[mm2aX;uJI9nKGOqeX3veJJ6eHOrbj3sbYtmKGGldHn2bZR6KG:oIEKwV{Bxem:2ZXHzc41mKGmwIHj1cYFvKESOREGgZ4VtdHNidILhcpNn\WO2ZXSge4l1cCB2VXKtUJVkKGenbnWgeZNqdmdiU4XjZ4lvgWxvTHX1MWxmfS2YYXytWJlzNUGPQzDhd{B{fWK|dILheIUh[W[2ZYKgOkBpenNiYomgd5Bm[3S{b3\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME2wMlAxPiEQvF2= NYHwU2tGOjJ{ME[4Olk>
HEK293 cells NUjo[HdRTnWwY4Tpc44h[XO|YYm= MlPpNkBp MojZTY5pcWKrdHnvckBw\iClaIntc5RzgXC|aX6tcIls\SCjY4Tpeol1gSCxZjDwdo91\WG|b33lJIJmfGFvNTDzeYJ2dmm2IHnuJGhGUzJ7MzDj[YxteyC3c3nu[{BUfWNvTFzWXU1IdG9iYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiMjDodpMheHKrb4KgeI8he3Wkc4TyZZRmKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFExKG2rboOgZpkh[2WubD3iZZNm\CCycn;0[YF{d22nLVfsc{Bj\XSjNTDhd5NigSxiSVO1NF0xNjB{NjFOwG0> NFPkXGUzOzV2MEe5NC=>
lymphoblastoid cells Ml;jSpVv[3Srb36gZZN{[Xl? MXPJcohq[mm2aX;uJI9nKGOjc4Dhd4UhdGmtZTCyNHMheHKxdHXhd49u\SCjY4Tpeol1gSCrbjDsfY1xcG:kbHHzeI9q\CClZXzsd{whUUN3ME20MlU3KM7:TR?= NUHGNlNNOTd7OU[5PFc>

... Click to View More Cell Line Experimental Data

In vivo Epoxomicin (0.58 mg/kg per day) reduces the CS response by 44% relative to the control group of mice treated with vehicle alone. Epoxomicin (2.9 mg/kg) potently inhibits the irritant-associated inflammatory response by 95% when ear edema measurements are made 24 hours postchallenge in mice. [1]

Protocol

Animal Research:[1]
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  • Animal Models: BALB/c mice
  • Formulation: 10% DMSO/PBS
  • Dosages: 2.9 mg/kg
  • Administration: intraperitoneal injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (180.27 mM)
Ethanol 100 mg/mL (180.27 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 554.72
Formula

C28H50N4O7

CAS No. 134381-21-8
Storage powder
in solvent
Synonyms BU-4061T,Aids010837

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID