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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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 MlzQVJJwdGmoZYLheIlwdiCjc4PhfS=> MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxtKGyrbnWsJGlEPTB;MD6wNFEh|ryP MWexOlY5PjV|Nx?=
WM266.4 cells NULpVHZmS3m2b4TvfIlkcXS7IHHzd4F6 MnXNO|IhcA>? NV:2VFY5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hX01{Nk[uOEBk\WyuczDh[pRmeiB5MjDodpMh[nliQWTQcIl1\SCjc4PhfUwhUUN3ME2wMlAxPDhizszN NFnPUY0zOjJyNki2PS=>
human LCL cells NEHwTotHfW6ldHnvckBie3OjeR?= M2m2b|EzKGh? NGfNemxKdmirYnn0bY9vKG:oIHPofY1wfHK7cIPpck1tcWunIHHjeIl3cXS7IH;mJFIxWyCycn;0[YF{d22nIHLleIEzKGmwIHj1cYFvKEyFTDDj[YxteyCjZoTldkAyOiCqcoOsJGlEPTB;MD6wNFUh|ryP NHLCZmMzODZ6N{[wPS=>
human DLD1 cells MXXGeY5kfGmxbjDhd5NigQ>? MlnkTY5pcWKrdHnvckBw\iClaIntc5RzgXC|aX6tcIls\SCjY4Tpeol1gSCxZjCyNHMheHKxdHXhd49u\SCrbjDoeY1idiCGTFSxJINmdGy|IITyZY5{\mWldHXkJJdqfGhiNGXiMWx2[yCpZX7lJJV{cW6pIGP1Z4NqdnmuLVzleU1N\XVvVnHsMXR6ei2DTVOgZZMhe3Wkc4TyZZRmKGGodHXyJFYhcHK|IHL5JJNx\WO2cn;mcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9NE4xODZizszN NG\SRpQzOjJyNki2PS=>
HEK293 cells NUjxSIlETnWwY4Tpc44h[XO|YYm= M1njdVIhcA>? NYHwXXYzUW6qaXLpeIlwdiCxZjDjbJlud3S{eYDzbY4udGmtZTDhZ5Rqfmm2eTDv[kBxem:2ZXHzc41mKGKndHGtOUB{fWK3bnn0JIlvKEiHS{K5N{Bk\WyuczD1d4lv\yCVdXOtUGxXYS2JbH:gZZMhe3Wkc4TyZZRmKGmwY4XiZZRm\CCob4KgNkBpenNicILpc5IhfG9ic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDFyIH3pcpMh[nliY3XscE1j[XOnZDDwdo91\WG|b33lMWdtdyCkZYThOUBie3OjeTygTWM2OD1yLkCyOkDPxE1? MWCyN|U1ODd7MB?=
lymphoblastoid cells NWnwXndRTnWwY4Tpc44h[XO|YYm= MV\Jcohq[mm2aX;uJI9nKGOjc4Dhd4UhdGmtZTCyNHMheHKxdHXhd49u\SCjY4Tpeol1gSCrbjDsfY1xcG:kbHHzeI9q\CClZXzsd{whUUN3ME20MlU3KM7:TR?= MkKxNVc6QTZ7OEe=

... 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