LDN 57444
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
LDN 57444是一种可逆的和竞争性的泛素C端水解酶L1(Uch-L1)抑制剂,IC50值为0.88 μM [1]。
除了Uch-L1,LDN 57444还抑制Uch-L3,IC50值为25 μM。对Uch酶的抑制可引起长时程增强和基础突触传递的减少,其效应与Aβ诱导的改变相似[1]。
在大鼠胰岛素瘤细胞系INS 832/13中,LDN 57444导致细胞凋亡。当LDN 57444的浓度高于30 μM时,可观察到caspase-3活性的增加。LDN 57444也诱导核CHOP,表明Uch-L1抑制所诱导的细胞凋亡与ER应激相关[2]。
参考文献:
[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.
Physical Appearance | A solid |
Storage | Desiccate at 4°C |
M.Wt | 397.64 |
Cas No. | 668467-91-2 |
Formula | C17H11Cl3N2O3 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥16.7 mg/mL in DMSO with gentle warming |
Chemical Name | [(Z)-[5-chloro-1-[(2,5-dichlorophenyl)methyl]-2-oxoindol-3-ylidene]amino] acetate |
SDF | Download SDF |
Canonical SMILES | CC(=O)ON=C1C2=C(C=CC(=C2)Cl)N(C1=O)CC3=C(C=CC(=C3)Cl)Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1,2]: | |
细胞系 |
大鼠胰岛瘤细胞系INS 832/13,SK-N-SH细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于16.7 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
30 μM,24 h |
应用 |
在大鼠胰岛瘤细胞系INS 832/13中,LDN 57444诱导细胞凋亡。LDN 57444(>30 μM)增加了caspase-3的活性。LDN 57444诱导核CHOP,表明细胞凋亡是通过抑制Uch-L1诱导的。在SK-N-SH细胞中,LDN 57444(25-100 μM)诱导SK-N-SH细胞的凋亡性细胞死亡。LDN 57444引发SK-N-SH细胞内质网应激。 |
动物实验 [1]: | |
动物模型 |
APP/PS1小鼠 |
给药剂量 |
腹腔注射,0.4 mg/kg |
应用 |
LDN 57444引起体内突触蛋白分布和脊柱形态的显著变化。LDN 57444导致Uch-L1活性迅速下降。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
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. |
描述 | LDN 57444是泛素C端水解酶L1(UCH-L1)的抑制剂,Ki值为0.4 μM。 | |||||
靶点 | UCH-L1 | |||||
IC50 | 0.4 μM (Ki) |
质量控制和MSDS
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