Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Epoxomicin (BU-4061T,Aids010837) 是一种含环氧酮的天然产物,可穿越血脑屏障,并具有很强的抗肿瘤和抗炎活性。它是一种选择性不可逆的蛋白酶体抑制剂,抑制类胰凝乳蛋白酶的活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,070 | 现货 | ||
5 mg | ¥ 3,180 | 现货 | ||
10 mg | ¥ 4,650 | 现货 | ||
25 mg | ¥ 7,370 | 现货 | ||
50 mg | ¥ 9,930 | 现货 | ||
100 mg | ¥ 13,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,930 | 现货 |
产品描述 | 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. |
体外活性 | 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] |
体内活性 | 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] |
别名 | BU-4061T, BU-4061T,Aids010837, 环氧酶素 |
分子量 | 554.72 |
分子式 | C28H50N4O7 |
CAS No. | 134381-21-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (167.7 mM)
Ethanol: 93 mg/mL (167.7 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.8027 mL | 9.0136 mL | 18.0271 mL | 45.0678 mL |
5 mM | 0.3605 mL | 1.8027 mL | 3.6054 mL | 9.0136 mL | |
10 mM | 0.1803 mL | 0.9014 mL | 1.8027 mL | 4.5068 mL | |
20 mM | 0.0901 mL | 0.4507 mL | 0.9014 mL | 2.2534 mL | |
50 mM | 0.0361 mL | 0.1803 mL | 0.3605 mL | 0.9014 mL | |
100 mM | 0.018 mL | 0.0901 mL | 0.1803 mL | 0.4507 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Epoxomicin 134381-21-8 Apoptosis Proteases/Proteasome Ubiquitination Proteasome inhibit BU-4061T covalently BBB cytotoxicities Inhibitor antitumor anti-inflammatory Parkinson's BU-4061T,Aids010837 antiproliferative 环氧酶素 Epoxyketone-containing inhibitor