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CAS No.: 418805-02-4

PYR-41 Catalog No. CSN15975

Synonyms: N/A

PYR-41 (50 μM) inhibits activity of ubiquitin-activating enzyme E1 by over 90%.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 E1 enzyme

IC50:10μM
描述Ubiquitin-activating enzyme (E1), ubiquitin-conjugating enzyme (E2) and ubiquitin protein ligase (E3) are the key enzymes in protein ubiquitylation. PYR-41 is a pyrazone derivative that selectively inhibits E1 with an IC₅₀ value less than 10 μM and a 95% inhibition was observed at the concentration of 50 μM. PYR-41 at 50 μM efficiently inhibited cyclin E degradation in vitro. PYR-41 reduced the level of E1∼Ub thioesters in retinal pigment epithelial cells with IC₅₀ values ranging from 10-25 μM. The exposure of retinal pigment epithelial cells with PYR-41 (50 μM) for 30 min also blocked the accumulation of ubiquitin conjugates in response to the proteasome inhibitor ALLN. In U2OS cells, treatment of PYR-41 (50 μM) for 8 hours inhibited ubiquitylation and proteasomal degradation of a test substrate. In HeLa cells treated with EGF (100 ng/mL), pretreatment with PYR-41 for 15 min decreased the ligand-induced EGFR ubiquitylation. PYR-41 at 50 μM also reduced NF-κB activation in Hela cells by inhibiting the ubiquitylation of upstream signaling molecules and by blocking the proteasomal degradation of IκBα^[3]. In a mouse model of cecal ligation and puncture (CLP)-induced sepsis, intravenous administration of PYR-41 (5 mg/kg) immediately after CLP significantly decreased serum levels of proinflammatory cytokines, including TNF-α, IL-1β, and IL-6, and the levels of organ injury markers, such as AST, ALT, and LDH. PYR-41 treatment also reduced myeloperoxidase activity and suppressed apoptosis and caspase-3 degradation in the lungs of septic mice as compared to DMSO-treated group. PYR-41 also significantly promoted 10-day survival in mice with sepsis from 42% to 83%^[4].
作用机制PYR-41 selectively inhibits E1 possibly by covalently modifying the active site cysteine of E1.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HI5 insect cells	-	Function assay	30 min	Inhibition of N-terminal GST-tagged human UAE-catalyzed UAE-Ub thioester intermediate formation expressed in HI5 insect cells after 30 mins by immunoblotting analysis, IC50=10 μM	23360215
HI5 insect cells	-	Function assay	-	Inhibition of N-terminal GST-tagged human UAE-catalyzed [32P]-AMP:[a-32P]-ATP exchange expressed in HI5 insect cells by TLC analysis, IC50=6.4 μM	23360215
insect cells	-	Function assay	-	Inhibition of mouse recombinant His6-tagged UAE-catalyzed UAE-Ub thioester intermediate formation expressed in insect cells by SDS-PAGE analysis, IC50=10 μM	23360215

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6932 mL
- 13.4662 mL
- 26.9323 mL
- 5 mM
- 0.5386 mL
- 2.6932 mL
- 5.3865 mL
- 10 mM
- 0.2693 mL
- 1.3466 mL
- 2.6932 mL

技术信息

CAS号

418805-02-4

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H13N3O7

运输

蓝冰

分子量

371.30

别名

N/A

溶解度

DMSO	52.0 mg/mL (140.0 mM)
Water	insoluble

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

2 mg/mL

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