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) can be used to induce animal models of Parkinson's Disease.

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)

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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.Epoxomicin (BU-4061T) can be used to induce animal models of Parkinson's Disease.
特性 Epoxomicin is a natural product isolated from an Actinomycetes species.
Targets
20S proteasome [1]
In Vitro
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]
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 (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, epoxomicin (BU-4061T; 10 μM), or vehicle control and then treated with saline or Ang II (100 nM) for 24 hours.
In Vivo
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]
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
  • 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/

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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