Epoxomicin (BU-4061T)

Catalog No.S7038 Batch:S703801

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Technical Data

Formula

C28H50N4O7
Molecular Weight 554.72 CAS No. 134381-21-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (180.27 mM)
Ethanol 100 mg/mL (180.27 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Epoxomicin (BU-4061T, Aids010837) 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. Epoxomicin promotes apoptosis.
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]
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]
Features Epoxomicin is a natural product isolated from an Actinomycetes species.

Protocol (from reference)

Kinase Assay:

[1]
  • Enzyme Kinetic Assays

    For proteasome inhibition assays, peptide-AMC substrates (5 μM Suc-LLVY-AMC, 5 μM Z-LLE-AMC, and 5 μM Boc-LRR-AMC) and Epoxomicin in DMSO are added to assay solutions at a final DMSO concentration of 1%. The following assay buffer is used: 20 mM Tris⋅HCl, pH 8.0/0.5 mM EDTA (plus 0.035% SDS for Suc-LLVY-AMC and Z-LLE-AMC assays). Bovine red blood cell proteasome is added to the assay buffer containing substrates and Epoxomicin at a final volume of 100 μL at room temperature (23℃) in a Dynex Microfluor II 96-well plate and the fluorescence emission immediately is measured at 460 nm (λex, 360 nM) by using a Cytofluor fluorescence plate reader for 50 min.
Cell Assay:

[6]
  • Cell lines

    LECs

  • Concentrations

    10 μM

  • Incubation Time

    24 h

  • Method

    LECs were pretreated with vehicle, losartan (10 μM), epoxomicin (10 μM), or vehicle control and then treated with saline or Ang II (100 nM) for 24 hours.
Animal Study:

[1]
  • Animal Models

    BALB/c mice

  • Dosages

    2.9 mg/kg

  • Administration

    intraperitoneal injection

Customer Product Validation

Data from [Data independently produced by , , Front Immunol, 2018, 9:1268]

Data from [Data independently produced by , , Front Immunol, 2018, 9:1231]

Selleck's Epoxomicin (BU-4061T) has been cited by 24 publications

The Ubiquitin-Proteasome System Facilitates Membrane Fusion and Uncoating during Coronavirus Entry [ Viruses, 2023, 15(10)2001] PubMed: 37896778
AurkA nuclear localization is promoted by TPX2 and counteracted by protein degradation [ Life Sci Alliance, 2023, 6(5)e202201726] PubMed: 36797043
A Protumorigenic mDia2-MIRO1 Axis Controls Mitochondrial Positioning and Function in Cancer-Associated Fibroblasts [ Cancer Res, 2022, 82(20):3701-3717] PubMed: 35997559
Angiotensin II Induces Cardiac Edema and Hypertrophic Remodeling through Lymphatic-Dependent Mechanisms [ Oxid Med Cell Longev, 2022, 2022:5044046] PubMed: 35222798
ATGL deficiency aggravates pressure overload-triggered myocardial hypertrophic remodeling associated with the proteasome-PTEN-mTOR-autophagy pathway [ Cell Biol Toxicol, 2022, 10.1007/s10565-022-09699-0] PubMed: 35218467
Chaperone-mediated Autophagy Regulates Cell Growth by Targeting SMAD3 in Glioma [ Neurosci Bull, 2022, 10.1007/s12264-022-00818-9] PubMed: 35267139
Galectin-1 and -3 in high amounts inhibit angiogenic properties of human retinal microvascular endothelial cells in vitro [ PLoS One, 2022, 17(3):e0265805] PubMed: 35320287
Hybrid Androgen Receptor Inhibitors Outperform Enzalutamide and EPI-001 in in vitro Models of Prostate Cancer Drug Resistance [ ChemMedChem, 2022, e202200548.] PubMed: 36300876
A heat-shock response regulated by the PfAP2-HS transcription factor protects human malaria parasites from febrile temperatures [ Nat Microbiol, 2021, 6(9):1163-1174] PubMed: 34400833
A Translocation Pathway for Vesicle-Mediated Unconventional Protein Secretion [ Cell, 2020, 30;181(3):637-652.e15.] PubMed: 32272059

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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