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1000313-40-5 | UK-101

UK-101 NLT 98%

SKU : MC500094

CAS Number : 1000313-40-5

Molecular Formula : C25H48N2O5Si | Molecular Weight : 484.74

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Purity NLT 98%
Storage at 20ºC 2 years

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Chemical Name UK-101
CAS Number 1000313-40-5
Molecular Formula C25H48N2O5Si
Molecular Weight 484.74
Introduction of 1000313-40-5 :

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]. IC50 & Target: IC50: 104 nM (LMP2)
IC50: 15 μM (immunoproteasome β1c)
IC50: 1 μM (immunoproteasome β5)[1] In Vitro: 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[2].
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[2].
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[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].

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