Epoxomicin (BU-4061T)

製品コードS7038 バッチS703801

印刷

化学情報

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 1 40%PEG300 2 5%Tween80 3 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）は、抗炎症作用を持つ選択的プロテアソーム阻害剤であり、主に20SプロテアソームのCH-L活性を阻害しますが、T-LおよびPGPH触媒活性も100〜1000倍低い速度で阻害されます。Epoxomicinはアポトーシスを促進します。Epoxomicin（BU-4061T）は、パーキンソン病の動物モデルを誘導するために使用できます。
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, inhibits IκBα degradation by 10-fold, and produces a significant dose-dependent reduction in TNF-α-stimulated NF-κB DNA-binding activity in the same cell line. It inhibits proliferating of EL4 lymphoma cells with biotinylated chimerae with IC50 of 4 nM. At 1 μM, it leads to a reduction of LCMV GP33 presentation and an enhancement of GP276 presentation. This compound inhibits growth of Babesia bigemina with IC50 of 4 nM. It (0.5 mg/kg and 0.05 mg/kg) results in peak parasitemia levels of 34.8% and 42.3% in B. microti. Epoxomicin (100 nM) decreases the total parasitemia by 78%, 86% and 77% in Plasmodium falciparum. At 10 μM, it inhibits gametogenesis and exflagellation as well as development into oocysts of anopheles mosquitoes.
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. This compound (2.9 mg/kg) potently inhibits the irritant-associated inflammatory response by 95% when ear edema measurements are made 24 hours postchallenge in mice.
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
キナーゼアッセイ	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/

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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
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

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。