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EPOXOMICIN(BU 4061T)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
EPOXOMICIN(BU 4061T)图片
CAS NO:134381-21-8
规格:≥98%
包装与价格：
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)554.72
FormulaC28H50N4O7
CAS No.134381-21-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (180.3 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (180.3 mM)
Other infoChemical Name: (2S,3S)-2-[[(2S,3S)-2-[Acetyl(methyl)amino]-3-methylpentanoyl]amino]-N-[(2S,3R)-3-hydroxy-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]-3-methylpentanamide
InChi Key: DOGIDQKFVLKMLQ-JTHVHQAWSA-N
InChi Code: InChI=1S/C28H50N4O7/c1-11-16(5)21(30-27(38)23(17(6)12-2)32(10)19(8)34)25(36)31-22(18(7)33)26(37)29-20(13-15(3)4)24(35)28(9)14-39-28/h15-18,20-23,33H,11-14H2,1-10H3,(H,29,37)(H,30,38)(H,31,36)/t16-,17-,18+,20-,21-,22-,23-,28+/m0/s1
SMILES Code: CC[C@H](C)[C@H](NC([C@@H](N(C(C)=O)C)[C@@H](C)CC)=O)C(N[C@@H]([C@H](O)C)C(N[C@@H](CC(C)C)C([C@]1(C)OC1)=O)=O)=O
SynonymsBU-4061T; BU 4061T; BU4061T; EPOXOMICIN;
实验参考方法
In Vitro

In vitro activity: 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. Epoxomicin inhibits proliferating of EL4 lymphoma cells with biotinylated chimerae with IC50 of 4 nM. Epoxomicin (1 μM) leads to a reduction of LCMV GP33 presentation and an enhancement of GP276 presentation.

In VivoEpoxomicin (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.
Animal modelBALB/c mice
Formulation & DosageDissolved in 10% DMSO/PBS; 2.9 mg/kg; i.p. injection
ReferencesProc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8.
生物活性

Accumulation of p53 (A) and ubiquitinated proteins (B) in epoxomicin-treated cells. Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8.

Epoxomicin inhibits activation of NF-κB. Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8.

Epoxomicin inhibits inflammation in vivo. Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8.