668467-91-2|LDN-57444|CsnPharm

CAS No.: 668467-91-2

LDN-57444 Catalog No. CSN18381

Synonyms: Ubiquitin C-terminal Hydrolase L1 Inhibitor;UCH-L1 Inhibitor

LDN-57444 is a reversible inhibitor of UCHL1 with IC50 of 0.88 μM (Ki = 0.4 μM) and its selectivity is better than UCH-L3 (IC50 = 25 μM).

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400-920-2911

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实验方案

技术信息

生物活性

描述Deubiquitinating enzymes (DUBs) function to remove covalently attached ubiquitin from proteins, thereby controlling substrate activity and/or abundance. The DUB ubiquitin carboxyl-terminal hydrolase L1 (UCH-L1) is a component of the ubiquitin proteasome system (UPS), it is abundantly expressed in neuronal brain cells and has been connected to Parkinson's disease (PD)^[3]. LDN-57444 is a specific inhibitor of UCH-L1 with IC50 value of 0.88 μM^[4]. In vitro, LDH-57444 treatment significantly inhibited proteasome activity in a concentration-dependent manner at 25 μM and above, and treatment with 50 μM LDH-5744 for 24h led to 70% inhibition of the proteasome activity in human neuroblastoma SK-N-SH cells. LDN-57444 greatly reduced the cell viability and induced apoptosis of SK-N-SH cells at concentration ranging in 25 – 100 μM^[5]. In vivo, LDN-57444 had an inhibitory effect on UCHL1 in the hippocampus at systemic doses of 0.5 mg/kg. Administration LDN-57444 at dose of 1 mg/kg for 4h significantly inhibited levels of free monomeric ubiquitin in mice. However, high dose LDN-57444 (2.5 mg/kg) increased UCHL1 expression, possibly as a compensatory mechanism. In addition, both 1 mg/kg and 2.5 mg/kg doses of LDN57444 depleted the hippocampus of postsynaptic density protein PSD95^[4].
动物研究
剂量
Mice: 0.5 mg/kg - 2.5 mg/kg^[3] (i.p.) Rat: 0.03 mg/kg^[4] (i.v.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Mice: 0.5 mg/kg - 2.5 mg/kg^[3] (i.p.) Rat: 0.03 mg/kg^[4] (i.v.)
给药途径	i.p., i.v.

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
- 2.5148 mL
- 12.5742 mL
- 25.1484 mL
- 5 mM
- 0.5030 mL
- 2.5148 mL
- 5.0297 mL
- 10 mM
- 0.2515 mL
- 1.2574 mL
- 2.5148 mL

技术信息

CAS号

668467-91-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H11Cl3N2O3

运输

蓝冰

分子量

397.64

别名

Ubiquitin C-terminal Hydrolase L1 Inhibitor;UCH-L1 Inhibitor

溶解度

DMSO	43.0 mg/mL (108.1 mM) warming
Water	insoluble

动物实验配方

5% DMSO+corn oil

6 mg/mL

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