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UK-101

Catalog No. T13247   CAS 1000313-40-5
Synonyms: UK101, UK 101

UK-101 is a potent and selective inhibitor of the immunoproteasome LMP2, inhibiting β1i (LMP2), β1c (LMP2), and β5 (LMP2), with IC50s of 104 nM, 15 μM, and 1 μM. UK-101 has a 144-fold and 10-fold higher affinity for β1i than for the distribution of β1c and β5 subunits. UK-101 induces apoptosis and can be used to study prostate cancer related diseases.

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UK-101 Chemical Structure
UK-101, CAS 1000313-40-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 410.00
5 mg In stock $ 963.00
10 mg In stock $ 1,290.00
25 mg In stock $ 1,860.00
50 mg In stock $ 2,380.00
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Purity: 99.58%
ee: 98.78%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description UK-101 is a potent and selective inhibitor of the immunoproteasome LMP2, inhibiting β1i (LMP2), β1c (LMP2), and β5 (LMP2), with IC50s of 104 nM, 15 μM, and 1 μM. UK-101 has a 144-fold and 10-fold higher affinity for β1i than for the distribution of β1c and β5 subunits. UK-101 induces apoptosis and can be used to study prostate cancer related diseases.
Targets&IC50 LMP2:104 nM, Immunoproteasome β1c:15 μM, Immunoproteasome β5:1 μM, Immunoproteasome β5:1 μM , LMP2:104 nM , Immunoproteasome β1c:15 μM
In vitro In the G1 phase of the cell cycle, UK-101 (2-8 μM; 24 hours) induces cell cycle arrest and increases the number of the PC-3 cell arrest.UK-101 (1-8 μM; 24 hours) induces cell accumulation in the G1 phase of the cell cycle, it increases p27 accumulation and significantly increases PARP cleavage as a dose-dependent manner.[1]
In vivo Tumor volume as a dose-dependent manner decreased by UK-101 (1-3 mg/kg; twice a week; 3 weeks)intraperitoneal injection, it significantly decreases tumor volume at a dose of 3 mg/kg. Additionally, UK-101-treated mice are suffering less systemic toxicity and the weights of mice treated with UK-101 remain steady over the 3-week treatment period.[1]
Synonyms UK101, UK 101
Molecular Weight 484.74
Formula C25H48N2O5Si
CAS No. 1000313-40-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (103.15 mM)

TargetMolReferences and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Active Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library

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Keywords

UK-101 1000313-40-5 Proteases/Proteasome Ubiquitination Proteasome UK101 UK 101 inhibitor inhibit

 

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