UK-101

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

一种有效的特异性免疫蛋白酶体 β1i (LMP2) 亚基抑制剂，IC50 为 104 nM。

A potent, specific immunoproteasome β1i (LMP2) subunit inhibitor with IC50 of 104 nM, 144- and 10-fold selectivity over β1c and β5 subunit respectivey; induces apoptosis of PC-3 cells and results in significant inhibition (~50-60%) of tumour growth in vivo, does not block degradation of IκBα in PC-3 cells treated with TNF-α.

UK-101 (2-8 μM; 24 hours) induces cell cycle arrest and increases the number of the PC-3 cells arrest in G1 phase of the cell cycle.UK-101 (2-8 μM; 24 hours) induces cell apoptosis, shows a minimal increase in late apoptosis, but has no significant increase in early apoptosis.UK-101 (1-8 μM; 24 hours) induces cells accumulation in the G1 phase of the cell cycle, it increases p27 accumulation and significantly increases?PARP cleavage as a dose-dependent manner. Cell Cycle Analysis Cell Line:PC-3 cells Concentration:2 μM; 8 μM Incubation Time:24 hours Result:Induced G1 cell cycle arrest in PC-3 cells. Apoptosis Analysis Cell Line:PC-3 cells Concentration:2 μM; 8 μM Incubation Time:24 hours Result:Increased cell apoptosis as a dose-dependent manner. Western Blot Analysis Cell Line:PC-3 cells Concentration:1 μM; 2 μM; 8 μM Incubation Time:24 hours Result:Increased PARP cleavage and p27 accumulation as a dose-dependent manner.

UK-101 (intraperitoneal injection; 1-3 mg/kg; twice a week; 3 weeks) decreases tumor volume as a dose-dependent manner, it significantly decreases tumor volume at a dose of 3 mg/kg. Additionally, UK-101-treated mice is suffering less systemic toxicity and the weights of mice treated with UK-101 remains steady over the 3-week treatment period. Animal Model:Subcutaneously implanted PC-3 cells in 6-week-old male BALB/c athymic nude mice Dosage:1 mg/kg; 3 mg/kg Administration:Intraperitoneal injection; twice a week; 3 weeks Result:Inhibited tumour growth in the prostate cancer mouse xenograft model.

UK 101 | UK101

Proteasome/Ubiquitin

Proteasome

Proteasome

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1000313-40-5

484.753

C25H48N2O5Si

>98% (HPLC)

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N-((S)-1-(((S)-1-((S)-2-(((tert-butyldimethylsilyl)oxy)methyl)oxiran-2-yl)-4-methyl-1-oxopentan-2-yl)amino)-1-oxopropan-2-yl)heptanamide

(-20℃)

With Ice Pack

≥ 2 years