Epoxomicin (BU-4061T)
别名: Aids010837 中文名称：环氧酶素
Epoxomicin (BU-4061T, Aids010837) 是一种选择性蛋白酶体抑制剂，具有抗炎活性，首要抑制20S蛋白酶体的CH-L活性，也抑制T-L和PGPH催化活性。Epoxomicin 可促进凋亡。
Epoxomicin (BU-4061T) Chemical Structure
CAS: 134381-21-8
产品质控
Epoxomicin (BU-4061T)相关产品
| 相关靶点 | 20S proteasome | 点击展开 |
|---|---|---|
| 相关产品 | MG132 Celastrol Oprozomib ONX-0914 (PR-957) Delanzomib VR23 Marizomib (Salinosporamide A) PI-1840 | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I 蛋白酶抑制剂库 泛素化化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Epoxomicin (BU-4061T, Aids010837) 是一种选择性蛋白酶体抑制剂，具有抗炎活性，首要抑制20S蛋白酶体的CH-L活性，也抑制T-L和PGPH催化活性。Epoxomicin 可促进凋亡。 | |
|---|---|---|
| 特性 | Epoxomicin是从Actinomycetes物种中分离的天然产物。 | |
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Epoxomicin共价结合到LMP7, X, MECL1，和蛋白酶体的Z催化亚基。Epoxomicin (100 nM)处理HUVECs，使p53蛋白水平增加30倍。Epoxomicin (10 μM)作用于HeLa细胞，导致泛素化蛋白累积。Epoxomicin(10 μM)作用于HeLa细胞，抑制IκBα降解。Epoxomicin(10 μM)作用于HeLa细胞，显著降低TNF-α刺激的NF-κB DNA结合活性，这种作用存在剂量依赖性。[1] Epoxomicin抑制EL4 淋巴瘤细胞增殖，IC50为4 nM。[2] Epoxomicin(1 μM) 降低LCMV GP33和增强 GP276。[3] Epoxomicin 抑制Babesia bigemina生长，IC50为4 nM。Epoxomicin按0.5 mg/kg和0.05 mg/kg剂量处理B. microti，虫血症峰值分别为34.8% 和42.3%。[4] Epoxomicin (100 nM)处理Plasmodium falciparum，降低78%, 86% 和77%虫血症。Epoxomicin (10 μM) 抑制配子和小配子形成按蚊的卵囊。[5] |
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|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 | Epoxomicin 每天按0.58 mg/kg剂量处理，与空白对照组小鼠相比，降低44% CS反应。Epoxomicin (2.9 mg/kg)处理小鼠，24小时后，测量耳肿胀，有效地抑制95％刺激性相关的炎症反应。[1] |
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|---|---|---|
| 动物实验 | Animal Models | BALB/c小鼠 |
| Dosages | 2.9 mg/kg | |
| Administration | 腹腔注射 | |
化学信息&溶解度
| 分子量 | 554.72 | 分子式 | C28H50N4O7 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (180.27 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL (180.27 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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