Home Proteases Proteasome inhibitor - Apoptosis related activator Epoxomicin (BU-4061T) For research use only.

Epoxomicin (BU-4061T)

Synonyms: Aids010837

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.

Epoxomicin (BU-4061T) Chemical Structure

Epoxomicin (BU-4061T) Chemical Structure

CAS No. 134381-21-8

Purity & Quality Control

Batch: S703801 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.87%
99.87

Epoxomicin (BU-4061T) Related Products

Signaling Pathway

Proteasome Signaling Pathways

Proteasome Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC3 Antiproliferative assay Antiproliferative activity against human PC3 cell line, IC50 = 0.001 μM. 16686537
WM266.4 Cytotoxicity assay 72 hrs Cytotoxicity against human WM266.4 cells after 72 hrs by ATPlite assay, IC50 = 0.0048 μM. 22206869
lymphoblastoid cells Function assay Inhibition of chymotrypsin like 20S proteasome activity in lymphoblastoid cells, IC50 = 0.005 μM. 17996987
LCL Function assay 12 hrs Inhibition of chymotrypsin-like activity of 20S proteasome beta2 in human LCL cells after 12 hrs, IC50 = 0.005 μM. 20687609
DLD1 Function assay 6 hrs Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis, IC50 = 0.006 μM. 22206869
HEK293 Function assay 2 hrs Inhibition of chymotrypsin-like activity of proteasome beta-5 subunit in HEK293 cells using Suc-LLVY-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta5 assay, IC50 = 0.026 μM. 23540790
DLD1 Function assay 6 hrs Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis, IC50 = 0.06 μM. 22206869
lymphoblastoid cells Function assay Inhibition of trypsin like 20S proteasome activity in lymphoblastoid cells, IC50 = 0.284 μM. 17996987
LCL Function assay 12 hrs Inhibition of trypsin-like activity of 20S proteasome beta2 in human LCL cells after 12 hrs, IC50 = 0.284 μM. 20687609
HEK293 Function assay 2 hrs Inhibition of postacid activity of 20s proteasome beta-1 subunit in HEK293 cells using Z-nLPnLD-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta1 assay, IC50 = 0.3 μM. 23540790
KB-8-5-11 Function assay P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen, Potency = 2.5929 μM. 31515284
lymphoblastoid cells Function assay Inhibition of caspase like 20S proteasome activity in lymphoblastoid cells, IC50 = 4.56 μM. 17996987
LCL Function assay 12 hrs Inhibition of PGPH catalytic activity of 20S proteasome beta2 in human LCL cells after 12 hrs, IC50 = 4.56 μM. 20687609
KB-3-1 Function assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
Click to View More Cell Line Experimental Data

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.
Features Epoxomicin is a natural product isolated from an Actinomycetes species.
Targets
20S proteasome [1]
In vitro
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]
Kinase Assay 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 Research Cell lines LECs
Concentrations 10 μM
Incubation Time 24 h
Method

LECs were pretreated with vehicle, epoxomicin (10 μM), or vehicle control and then treated with saline or Ang II (100 nM) for 24 hours.
In Vivo
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]
Animal Research Animal Models BALB/c mice
Dosages 2.9 mg/kg
Administration intraperitoneal injection

Chemical Information & Solubility

Molecular Weight 554.72 Formula

C28H50N4O7
CAS No. 134381-21-8 SDF Download Epoxomicin (BU-4061T) SDF
Smiles CCC(C)C(C(=O)NC(C(C)O)C(=O)NC(CC(C)C)C(=O)C1(CO1)C)NC(=O)C(C(C)CC)N(C)C(=O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (180.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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