LDN-57444, Ubiquitin C-terminal Hydrolase-L1 (UCH-L1) Inhibitor


Catalog No. size PriceQuantity
M60204-2S 2mg solid $79
M60204-10S 10mg solid $316

Description

Product Information
Molecular Weight: 397.64
Formula: C17H11Cl3N2O3
Purity: ≥98%
CAS#: 668467-91-2
Solubility: DMSO up to 25 mM
Chemical Name: (Z)-3-(acetoxyimino)-5-chloro-1-(2,5-dichlorobenzyl)indolin-2-one
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

LDN-57444 is a novel potent and selective inhibitor of ubiquitin C-terminal hydrolase-L1 (UCH-L1) with IC50 ~0.88 μM. It has ~28-fold greater selectivity over UCH-L3 (ubiquitin C-terminal hydrolase L3).  LDN-57444 can increase levels of highly ubiquitinated proteins and decreases ubiquitin proteasome activity. It causes cell death through the apoptosis pathway. LDN-57444’s activity leads to dramatic alterations in synaptic protein distribution and spine morphology in vivo.

 

How to Use:

 

  • In vitro:  LDN-57444 was used at 5-25 µM final concentration in various in vitro assays.
  • In vivo:  LDN-57444 was administered through IP injection at 0.5 mg/kg in a-syn transgenic mice.

 

 

Reference:

  • 1. Gong B, et al. Ubiquitin hydrolase Uch-L1 rescues beta-amyloid-induced decreases in synaptic function and contextual memory. (2006) Cell. 126(4):775-88.
  • 2. Liu Y, et al. Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line. (2003) Chem Biol. 10(9):837-46.
  • 3. Tan YY, et al. Endoplasmic reticulum stress contributes to the cell death induced by UCH-L1 inhibitor. (2008) Mol Cell Biochem. 318(1-2):109-15.
  • 4. Cartier AE, et al. Regulation of synaptic structure by ubiquitin C-terminal hydrolase L1. (2009) J Neurosci. 29(24):7857-68. 

 

  

Products are for research use only. Not for human use.

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