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S80286

Epoxomicin

源叶(MedMol) 99%
  • 英文名:
  • Epoxomicin
  • 别名:
  • 艾泼米辛;BU-4061T;EPOXOMICIN, N-乙酰基-N-甲基-L-异亮氨酰-L-异亮氨酰-N-[(1S)-3-甲基-1-[[(2R)-2-甲基-2-环氧乙烷基]羰基]丁基]-L-苏氨酰胺
  • CAS号:
  • 134381-21-8
  • 分子式:
  • C28H50N4O7
  • 分子量:
  • 554.719
  • 核磁/质谱:
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源叶(MedMol) S80286-1mg 99% ¥470.00元 2 - - - EA 加入购物车
源叶(MedMol) S80286-5mg 99% ¥1470.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S80286-10mg 99% ¥2800.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity
  • 靶点: Proteasome;Apoptosis;Proteasome
  • 体内研究:
    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.
  • 参考文献:
    1. Hanada M, et al. Epoxomicin, a new antitumor agent of microbial origin. J Antibiot (Tokyo). 1992 Nov;45(11):1746-52. 2. Kim KB, et al. Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency. Bioorg Med Chem Lett. 1999 Dec 6;9(23):3335-40. 3. Meng L, et al. Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity. Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8. 4. McNaught KS, et al. Systemic exposure to proteasome inhibitors causes a progressive model of Parkinson's disease. Ann Neurol. 2004 Jul;56(1):149-62. 5. Garrett IR, et al. Selective inhibitors of the osteoblast proteasome stimulate bone formation in vivo and in vitro. J Clin Invest. 2003 Jun;111(11):1771-82.
  • 溶解性: DMSO  :  100  mg/mL  (180.27  mM;  Need  ultrasonic)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.803 ml 9.014 ml 18.027 ml
    5 mM 0.361 ml 1.803 ml 3.605 ml
    10 mM 0.18 ml 0.901 ml 1.803 ml
    50 mM 0.036 ml 0.18 ml 0.361 ml
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