| Identification | Back Directory | [Name]
UK-101 | [CAS]
1000313-40-5 | [Synonyms]
UK-101
Heptanamide, N-[(1S)-2-[[(1S)-1-[[(2S)-2-[[[(1,1-dimethylethyl)dimethylsilyl]oxy]methyl]-2-oxiranyl]carbonyl]-3-methylbutyl]amino]-1-methyl-2-oxoethyl]- | [Molecular Formula]
C25H48N2O5Si | [MDL Number]
MFCD34469255 | [MOL File]
1000313-40-5.mol | [Molecular Weight]
484.74 |
| Chemical Properties | Back Directory | [Boiling point ]
624.9±55.0 °C(Predicted) | [density ]
1.009±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
13.33±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor. UK-101 induces cell apoptosis and can be used for the study of prostate cancer. | [Uses]
UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey[1]. UK-101 induces cell apoptosis and can be used for the study of prostate cancer[2]. | [in vivo]
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[2]. | Animal Model: | Subcutaneously implanted PC-3 cells in 6-week-old male BALB/c athymic nude mice[2] | | 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. |
| [References]
[1] de Bruin G, et al. Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. J Med Chem.?2014?Jul 24;57(14):6197-209. DOI:10.1021/jm500716s
[2] Wehenkel M, et al. A selective inhibitor of the immunoproteasome subunit LMP2 induces apoptosis in PC-3 cells and suppresses tumour growth in nude mice. Br J Cancer.?2012?Jun 26;107(1):53-62. DOI:10.1038/bjc.2012.243 |
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