1. Metabolic Enzyme/Protease
    Apoptosis
  2. Proteasome
    Apoptosis
  3. UK-101

UK-101 

Cat. No.: HY-119037
Handling Instructions

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. UK-101 induces cell apoptosis and can be used for the study of prostate cancer.

For research use only. We do not sell to patients.

UK-101 Chemical Structure

UK-101 Chemical Structure

CAS No. : 1000313-40-5

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Description

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].

Cell Cycle Analysis[1]

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[1]

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[1]

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.
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.
Molecular Weight

484.74

Formula

C₂₅H₄₈N₂O₅Si

CAS No.

1000313-40-5

SMILES

O=C([[email protected]]1(CO1)CO[Si](C)(C)C(C)(C)C)[[email protected]](CC(C)C)NC([[email protected]](C)NC(CCCCCC)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

UK-101UK101UK 101ProteasomeApoptosisapoptosispc-3celltumorcancerprostateantitumourDU 145LNCaPMCF7MDA-MB-231Inhibitorinhibitorinhibit

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UK-101
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