1000313-40-5
1000313-40-5 structure
- Name:
- Chemical Name:
- CAS Number: 1000313-40-5
- Molecular Formula: C25H48N2O5Si
- Molecular Weight: 484.74500
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2018-03-13 16:06:36
- Modify Date: 2024-01-06 12:34:48
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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].
| No information of Name |
| 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]. |
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| Related Catalog | |
| 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. |
| References |
| Molecular Formula | C25H48N2O5Si |
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| Molecular Weight | 484.74500 |
| Exact Mass | 484.33300 |
| PSA | 97.03000 |
| LogP | 5.13410 |