ホームページ Proteases Proteasome inhibitor - Apoptosis related activator Epoxomicin (BU-4061T) For research use only.

Epoxomicin (BU-4061T)

別名：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)化学構造

CAS No. 134381-21-8

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 101800 国内在庫あり
JPY 28000 国内在庫あり
JPY 86500 国内在庫あり
JPY 265500 国内在庫なし(納期7~10日)
JPY 568500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例（23）

カスタマーフィードバック2个实验数据

製品安全説明書

現在のバッチを見る： S703801 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false 純度： 99.87%
99.87

Epoxomicin (BU-4061T)関連製品

シグナル伝達経路

Proteasome Signaling Pathways

Proteasomeシグナル伝達経路

Proteasome阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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
WM266.4 Cytotoxicity assay 72 hrs Cytotoxicity against human WM266.4 cells after 72 hrs by ATPlite assay, IC50 = 0.0048 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
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
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
lymphoblastoid cells Function assay Inhibition of chymotrypsin like 20S proteasome activity in lymphoblastoid cells, IC50 = 0.005 μM. 17996987
PC3 Antiproliferative assay Antiproliferative activity against human PC3 cell line, IC50 = 0.001 μM. 16686537
lymphoblastoid cells Function assay Inhibition of trypsin like 20S proteasome activity in lymphoblastoid cells, IC50 = 0.284 μM. 17996987
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
KB-3-1 Function assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
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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.
特性 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.
細胞実験 細胞株 LECs
濃度 10 μM
反応時間 24 h
実験の流れ

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.
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]
動物実験 動物モデル BALB/c mice
投与量 2.9 mg/kg
投与経路 intraperitoneal injection

化学情報

分子量 554.72 化学式

C28H50N4O7
CAS No. 134381-21-8 SDF Download Epoxomicin (BU-4061T) SDFをダウンロードする
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
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (180.27 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 100 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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