Epoxomicin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Epoxomicin 是一种具有抗炎活性的选择性蛋白酶体抑制剂，主要抑制 20S 蛋白酶体的 CH-L 活性。

Epoxomicin is an irreversible, selective proteasome inhibitor.

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.

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.

Epoxomicin |

Others

Other Targets

20S proteasome

Cancer

——

134381-21-8

554.72

C28H50N4O7

>98% (HPLC)

DMSO : 100 mg/mL 180.27 mM;

CC[C@H](C)[C@H](NC(=O)[C@H]([C@@H](C)CC)N(C)C(C)=O)C(=O)NC(=O)[C@@H](N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1)[C@@H](C)O

(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

(-20℃)

With Ice Pack

≥ 2 years