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编 号:F127841
分子式:C28H50N4O7
分子量:554.72
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
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.

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.Animal Model:Male BDFX mice with B16 melanoma
Dosage:0.063 mg/kg, 0.13 mg/kg, 0.25 mg/kg, 0.5 mg/kg, 1 mg/kg
Administration:Intraperitoneal injection; once daily; for 9 days
Result:Exhibited strong therapeutic activity against B16 melanoma.

体外研究:
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.
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