Epoxomicin (BU-4061T)

製品コードS7038 バッチS703801

印刷

化学情報

Chemical Structure Synonyms Aids010837 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C28H50N4O7
分子量 554.72 CAS No. 134381-21-8
Solubility (25°C)* 体外 DMSO 100 mg/mL (180.27 mM)
Ethanol 100 mg/mL (180.27 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (9.01mM) 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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) can be used to induce animal models of Parkinson's Disease.
in vitro

Epoxomicin (BU-4061T) covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome. This compound (100 nM) results in a 30-fold increase in the levels of p53 protein, a known target of the proteasome, in HUVECs. It (10 μM) results in the accumulation of ubiquitinated proteins in HeLa cells and inhibits IκBα degradation by 10-fold in the same cell line. It (10 μM) also 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]

At 1 μM, it leads to a reduction of LCMV GP33 presentation and an enhancement of GP276 presentation. [3]

It inhibits growth of Babesia bigemina with IC50 of 4 nM. When administered at 0.5 mg/kg and 0.05 mg/kg, it results in peak parasitemia levels of 34.8% and 42.3% in B. microti. [4]

At 100 nM, it decreases the total parasitemia by 78%, 86% and 77% in Plasmodium falciparum. It (10 μM) inhibits gametogenesis and exflagellation as well as development into oocysts of anopheles mosquitoes. [5]
in vivo

Epoxomicin (BU-4061T) (0.58 mg/kg per day) reduces the CS response by 44% relative to the control group of mice treated with vehicle alone. It (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]
特徴 Epoxomicin is a natural product isolated from an Actinomycetes species.

プロトコル(参考用のみ)

キナーゼアッセイ 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 (BU-4061T) 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 this compound 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.
細胞アッセイ 細胞株 LECs
濃度 10 μM
反応時間 24 h
実験の流れ

LECs were pretreated with vehicle, epoxomicin (BU-4061T; 10 μM), or vehicle control and then treated with saline or Ang II (100 nM) for 24 hours.
動物実験 動物モデル BALB/c mice
投薬量 2.9 mg/kg
投与方法 intraperitoneal injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/10468620/
  • https://pubmed.ncbi.nlm.nih.gov/10612595/
  • https://pubmed.ncbi.nlm.nih.gov/10843664/
  • https://pubmed.ncbi.nlm.nih.gov/19896277/
  • https://pubmed.ncbi.nlm.nih.gov/19651911/

カスタマーフィードバック

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

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Activation of endogenous PRKN by structural derepression is linked to increased turnover of the E3 ubiquitin ligase [ Autophagy, 2025, 1-21.] PubMed: 40624741
Bi-allelic KICS2 mutations impair KICSTOR complex-mediated mTORC1 regulation, causing intellectual disability and epilepsy [ Am J Hum Genet, 2025, 112(2):374-393] PubMed: 39824192
The parkin V380L variant is a genetic modifier of Machado-Joseph disease with impact on mitophagy [ Acta Neuropathol, 2024, 148(1):14] PubMed: 39088078
Immunosuppressive MDSC and Treg signatures predict prognosis and therapeutic response in glioma [ Int Immunopharmacol, 2024, 141:112922] PubMed: 39137632
The Ubiquitin-Proteasome System Facilitates Membrane Fusion and Uncoating during Coronavirus Entry [ Viruses, 2023, 15(10)2001] PubMed: 37896778
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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