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CAS No. : 134381-21-8
MCE 国际站:Epoxomicin
产品活性:Epoxomicin (BU-4061T) 是一种含环氧酮的天然产物,是一种有效的,选择性的和不可逆的蛋白酶体 (proteasome) 抑制剂。Epoxomicin 与蛋白酶体的 LMP7,X,MECL1 和 Z 催化亚基共价结合,并有效地主要抑制类胰凝乳蛋白酶的活性。Epoxomicin 可以穿越血脑屏障,并具有很强的抗肿瘤和抗炎活性。
研究领域:Metabolic Enzyme/Protease | Apoptosis
作用靶点:Proteasome | Apoptosis
结构分类:酮、醛、酸
In Vitro: Epoxomicin shows quite potent cytotoxicities against all of the cells tested. Epoxomicin inhibits the cells growth of B16-F10, HCT116, Moser, P388 and K562 cells of IC50 values of 0.002 μg/mL, 0.005 μg/mL, 0.044 μg/mL, 0.002 μg/mL and 0.037 μg/mL.
Epoxomicin has antiproliferative activity with an IC50 of 4 nM in EL4 lymphoma cells.
In Vivo: Epoxomicin (0.063-1 mg/kg; intraperitoneal injection; once daily; for 9 days; male BDFX mice) treatment shows significant antitumor effect with the minimumeffective dose of 0.13mg/kg/day.
Epoxomicin also effectively inhibits NF-κB activation in vitro and potently blocks in vivo inflammation in the murine ear edema assay.
Epoxomicin is injected into adult rats over a period of 2 weeks. After a latency of 1 to 2 weeks, animals developed progressive Parkinsonism with bradykinesia, rigidity, tremor, and an abnormal posture. Postmortem analyses shows striatal dopamine depletion and dopaminergic cell death with apoptosis in the substantia nigra pars compacta.
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热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-13821
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