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抑制剂/激活剂

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凋亡与自噬

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Epoxomicin 环氧酶素

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。Epoxomicin (BU-4061T) 可用于诱导帕金森病动物模型。

货号：
TK0161
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	134381-21-8
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.
分子式	C28H50N4O7
分子量	554.72
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder, -20°C ,3 years
溶解性数据	DMSO : 100 mg/mL (180.27 mM; Need ultrasonic)
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.
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.
纯度及产品资料	98%

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