LDN 57444
(Synonyms: Ubiquitin C-terminal Hydrolase L1 Inhibitor, UCHL1 Inhibitor) 目录号 : GC10510
An inhibitor of UCH-L1
Cas No.:668467-91-2
Sample solution is provided at 25 µL, 10mM.
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LDN 57444 is a reversible competitive inhibitor of ubiquitin C-terminal hydrolase L1 (Uch-L1) with IC50 value of 0.88μM [1].
Besides Uch-L1, LDN 57444 also inhibits Uch-L3 with a higher IC50 value of 25μM. The inhibition of Uch enzymes subsequently causes the reduction of long-term potentiation and basal synaptic transmission, which is similar to the alterations induced by Aβ [1].
In rat insulinoma cell line INS 832/13, treatment of LDN 57444 leads to the cell apoptosis. The increased activity of caspase-3 can be seen when the concentration of LDN 57444 is above 30μM. LDN 57444 also induces nuclear CHOP, suggesting that the apoptosis induced by the inhibition of Uch-L1 is related to ER stress [2].
References:
[1] Gong B, Cao Z, Zheng P, Vitolo OV, Liu S, Staniszewski A, Moolman D, Zhang H, Shelanski M, Arancio O. Ubiquitin hydrolase Uch-L1 rescues beta-amyloid-induced decreases in synaptic function and contextual memory. Cell. 2006 Aug 25;126(4):775-88.
[2] Gong B, Cao Z, Zheng P, Vitolo OV, Liu S, Staniszewski A, Moolman D, Zhang H, Shelanski M, Arancio O. Ubiquitin hydrolase Uch-L1 rescues beta-amyloid-induced decreases in synaptic function and contextual memory. Cell. 2006 Aug 25;126(4):775-88.
| Cell experiment [1,2]: | |
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Cell lines |
Rat insulinoma cell line INS 832/13, SK-N-SH cells |
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Preparation method |
The solubility of this compound in DMSO is >16.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
30 μM, 24 h |
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Applications |
In rat insulinoma cell line INS 832/13, LDN 57444 induced cell apoptosis. LDN 57444 (>30 μM) increased the activity of caspase-3. LDN 57444 induced nuclear CHOP, suggesting that the apoptosis induced by the inhibition of Uch-L1. In SK-N-SH cells, LDN 57444 (25-100 μM) induced apoptotic cell death in SK-N-SH cells. LDN 57444 triggered the endoplasmic reticulum stress in SK-N-SH cells. |
| Animal experiment [1]: | |
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Animal models |
APP/PS1 Mice |
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Dosage form |
Intraperitoneal injection, 0.4 mg/kg |
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Application |
LDN 57444 caused dramatic alterations in synaptic protein distribution and spine morphology in vivo. Treatment with LDN 57444 resulted in a rapid fall of Uch-L1 activity. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Gong B, Cao Z, Zheng P, et al. Ubiquitin hydrolase Uch-L1 rescues β-amyloid-induced decreases in synaptic function and contextual memory[J]. Cell, 2006, 126(4): 775-788. [2]. Tan Y Y, Zhou H Y, Wang Z Q, et al. Endoplasmic reticulum stress contributes to the cell death induced by UCH-L1 inhibitor[J]. Molecular and cellular biochemistry, 2008, 318(1-2): 109-115. | |
| Cas No. | 668467-91-2 | SDF | |
| 别名 | Ubiquitin C-terminal Hydrolase L1 Inhibitor, UCHL1 Inhibitor | ||
| 化学名 | [(Z)-[5-chloro-1-[(2,5-dichlorophenyl)methyl]-2-oxoindol-3-ylidene]amino] acetate | ||
| Canonical SMILES | CC(=O)ON=C1C2=C(C=CC(=C2)Cl)N(C1=O)CC3=C(C=CC(=C3)Cl)Cl | ||
| 分子式 | C17H11Cl3N2O3 | 分子量 | 397.64 |
| 溶解度 | ≥ 16.7 mg/mL in DMSO with gentle warming | 储存条件 | Desiccate at 4°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5148 mL | 12.5742 mL | 25.1484 mL |
| 5 mM | 0.503 mL | 2.5148 mL | 5.0297 mL |
| 10 mM | 0.2515 mL | 1.2574 mL | 2.5148 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet