Epoxomicin

For research use only. Not for use in humans.

目录号:S7038 别名: BU-4061T,Aids010837 中文名称:环氧酶素

Epoxomicin Chemical Structure

CAS No. 134381-21-8

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。

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客户使用Selleck生产的Epoxomicin发表文献13篇:

客户使用该产品的2个实验数据:

  • Epoxomicin did not inhibit the EV71-induced PMLIII and IV degradation. Cell lysates were prepared from 293T cells infected or mock-infected with EV71 at a multiplicity of infection (MOI) of 5 for 24 or 48 h in the presence or absence of epoxomicin (1 µM). At 24 h post-infection (p.i.) (left panels) or 48 h p.i. (right panels), 60 μg of protein extracted from each treatment were separated on SDS-PAGE and analyzed by performing a Western blot analysis using antibodies specific for PMLIII and IV (top panels), VP1 (middle panels), and GAPDH, which served as an internal loading control (bottom panels). PMLIII and IV were quantified by performing densitometry and are presented relative to the mock infection, which was set as 1.0. VP1 was quantified and is presented relative to that in the EV71-infected 293T cells at 24 h p.i. (left panels) or 48 h p.i. (right panels). The density value of VP1 without epoxomicin is set as 1.0. The experiment was performed three times, and representative results are shown.

    Front Immunol, 2018, 9:1268. Epoxomicin purchased from Selleck.

  • Immature monocyte-derived dendritic cells (moDCs) were incubated 30 min prior and during the 3 h antigen (gp100/AZN-D1) pulse with 0.1% DMSO (vehicle), chloroquine (25 µM), MG132 (10 µM), epoxomicin (0.25 µM), and cathepsin S inhibitor (5 µM). Groups are significantly different compared to AZN-D1.

    Front Immunol, 2018, 9:1231. Epoxomicin purchased from Selleck.

产品安全说明书

Proteasome抑制剂选择性比较

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
20S proteasome [1]
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC3 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M4rwd2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGxibHnu[UwhUUN3MDC9JFAvODBzIN88UU4> M3zMRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4Nki2OVM4Lz5zNk[4OlU{PzxxYU6=
WM266.4 MoHTR5l1d3SxeHnjbZR6KGG|c3H5 NHXLeHM4OiCqcoO= MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDXUVI3Pi52IHPlcIx{KGGodHXyJFczKGi{czDifUBCXFCuaYTlJIF{e2G7LDDJR|UxKD1iMD6wNFQ5KM7:TT6= MnT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{ME[4OlkoRjJ{MkC2PFY6RC:jPh?=
lymphoblastoid cells NFjrdHFHfW6ldHnvckBie3OjeR?= NGDCSFJKdmirYnn0bY9vKG:oIHPofY1wfHK7cIPpckBtcWunIEKwV{Bxem:2ZXHzc41mKGGldHn2bZR6KGmwIHz5cZBpd2KuYYP0c4llKGOnbHzzMEBKSzVyIE2gNE4xODVizszNMi=> MknsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd7OU[5PFcoRjF5OUm2PVg4RC:jPh?=
LCL NHnNVlBHfW6ldHnvckBie3OjeR?= NVjhfpVpOTJiaILz NYfUT5ZbUW6qaXLpeIlwdiCxZjDjbJlud3S{eYDzbY4udGmtZTDhZ5Rqfmm2eTDv[kAzOFNicILveIVie2:vZTDi[ZRiOiCrbjDoeY1idiCOQ1ygZ4VtdHNiYX\0[ZIhOTJiaILzMEBKSzVyIE2gNE4xODVizszNMi=> M1HtbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNki3OlA6Lz5{ME[4O|YxQTxxYU6=
DLD1 NYW0RoFoTnWwY4Tpc44h[XO|YYm= NWLKfld[PiCqcoO= NULFXHo6UW6qaXLpeIlwdiCxZjDjbJlud3S{eYDzbY4udGmtZTDhZ5Rqfmm2eTDv[kAzOFNicILveIVie2:vZTDpckBpfW2jbjDEUGQyKGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigOHVjNUy3YzDn[Y5mKHW|aX7nJHN2[2OrbonsMWxmfS2OZYWtWoFtNVS7cj3BUWMh[XNic4Xid5Rz[XSnIHHmeIVzKDZiaILzJIJ6KHOyZXP0do9ndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVAhRSByLkCwOkDPxE1w M2jLSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkC2PFY6Lz5{MkKwOlg3QTxxYU6=
HEK293 MWPGeY5kfGmxbjDhd5NigQ>? MoDTNkBpenN? Mn7pTY5pcWKrdHnvckBw\iClaIntc5RzgXC|aX6tcIls\SCjY4Tpeol1gSCxZjDwdo91\WG|b33lJIJmfGFvNTDzeYJ2dmm2IHnuJGhGUzJ7MzDj[YxteyC3c3nu[{BUfWNvTFzWXU1IdG9iYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiMjDodpMheHKrb4KgeI8he3Wkc4TyZZRmKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFExKG2rboOgZpkh[2WubD3iZZNm\CCycn;0[YF{d22nLVfsc{Bj\XSjNTDhd5NigSxiSVO1NEA:KDBwMEK2JO69VS5? M2LITFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwO|kxLz5{M{W0NFc6ODxxYU6=
DLD1 MX7GeY5kfGmxbjDhd5NigQ>? NYrFd3ZSPiCqcoO= NH7VU|BKdmirYnn0bY9vKG:oIIDldJRq\GVvZ3z1eIFugWxvcHXweIll\S2qeXTyc4x6gmmwZzDhZ5Rqfmm2eTDv[kAzOFNicILveIVie2:vZTDpckBpfW2jbjDEUGQyKGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigOHVjNUy3YzDn[Y5mKHW|aX7nJHouVGW3LVzleU1IdHVvQV3DJIF{KHO3YoP0doF1\SCjZoTldkA3KGi{czDifUB{eGWldILv[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwJF0hOC5yNjFOwG0v M3SwO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkC2PFY6Lz5{MkKwOlg3QTxxYU6=
lymphoblastoid cells M{Hzc2Z2dmO2aX;uJIF{e2G7 NEPNcZhKdmirYnn0bY9vKG:oIITyfZB{cW5ibHnr[UAzOFNicILveIVie2:vZTDhZ5Rqfmm2eTDpckBtgW2yaH;icIF{fG:rZDDj[YxteyxiSVO1NEA:KDBwMki0JO69VS5? NVu0PJpORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe5PVY6QDdpPkG3PVk3QTh5PD;hQi=>
LCL MorhSpVv[3Srb36gZZN{[Xl? MVqxNkBpenN? NVfFWYNxUW6qaXLpeIlwdiCxZjD0dplxe2mwLXzpb4Uh[WO2aY\peJkhd2ZiMkDTJJBzd3SnYYPvcYUh[mW2YUKgbY4hcHWvYX6gUGNNKGOnbHzzJIFnfGW{IEGyJIhzeyxiSVO1NEA:KDBwMki0JO69VS5? M37LZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNki3OlA6Lz5{ME[4O|YxQTxxYU6=
HEK293 NVXGZmN5TnWwY4Tpc44h[XO|YYm= NIDQdnYzKGi{cx?= M{HkUGlvcGmkaYTpc44hd2ZicH;zeIFkcWRiYXP0bZZqfHlib3[gNlB{KHC{b4TlZZNwdWViYnX0ZU0yKHO3YoXubZQhcW5iSFXLNlk{KGOnbHzzJJV{cW6pIGqtcmxRdkyGLVfsc{BieyC|dXLzeJJifGViaX7jeYJifGWmIH\vdkAzKGi{czDwdolweiC2bzDzeYJ{fHKjdHWgZYRlcXSrb36gcYVie3W{ZXSgZYZ1\XJiMUCgcYlveyCkeTDj[YxtNWKjc3XkJJBzd3SnYYPvcYUuT2yxIHLleIEyKGG|c3H5MEBKSzVyIE2gNE4{KM7:TT6= NXT4e|NHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA4QTBpPkKzOVQxPzlyPD;hQi=>
KB-8-5-11 NUHw[pNUTnWwY4Tpc44h[XO|YYm= MmG4VE1odHmlb4Dyc5RmcW5ic4Xid5Rz[XSnczDp[IVvfGmoaXXkJIlvKEuELUitOU0yOSCjZHXuc4NiemOrbn;tZUBk\WyuIHzpcoUtKHGKVGOgeIhmemGyZYX0bYMhdGmkcnHyfUB{[3KnZX6sJHBwfGWwY4mgQUAzNjV7Mkmg{txONg>? MnjjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3MUWyPFQoRjNzNUG1Nlg1RC:jPh?=
lymphoblastoid cells NIO1fm9HfW6ldHnvckBie3OjeR?= NYrsRotIUW6qaXLpeIlwdiCxZjDjZZNx[XOnIHzpb4UhOjCVIIDyc5Rm[XOxbXWgZYN1cX[rdImgbY4hdHmvcHjvZoxie3SxaXSgZ4VtdHNuIFnDOVAhRSB2LkW2JO69VS5? M{C4c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5OUm2PVg4Lz5zN{m5Olk5PzxxYU6=
LCL MkXqSpVv[3Srb36gZZN{[Xl? NU[1b25MOTJiaILz MUHJcohq[mm2aX;uJI9nKFCJUFigZ4F1[Wy7dHnjJIFkfGm4aYT5JI9nKDJyUzDwdo91\WG|b33lJIJmfGF{IHnuJIh2dWGwIFzDUEBk\WyuczDh[pRmeiBzMjDodpMtKEmFNUCgQUA1NjV4IN88UU4> NVLJUpFmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2PFc3ODlpPkKwOlg4PjB7PD;hQi=>
KB-3-1 MmHnSpVv[3Srb36gZZN{[Xl? MXzQMYdtgWOxcILveIVqdiC|dXLzeJJifGW|IHnk[Y51cW[rZXSgbY4hU0JvMz2xJIFl\W6xY3HyZ4lvd22jIHPlcIwhdGmwZTygdWhVWyC2aHXyZZBmfXSrYzDsbYJz[XK7IIPjdoVmdg>? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTVzNUK4OEc,OzF3MUWyPFQ9N2F-

... Click to View More Cell Line Experimental Data

体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[1]
- 合并
  • Animal Models: BALB/c小鼠
  • Dosages: 2.9 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (180.27 mM)
Ethanol 100 mg/mL (180.27 mM)
Water Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 554.72
化学式

C28H50N4O7

CAS号 134381-21-8
储存条件 粉状
溶于溶剂
别名 BU-4061T,Aids010837

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

Proteasome Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID