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

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.

Product information

CAS Number: 668467-91-2

Molecular Weight: 397.64

Formula: C17H11Cl3N2O3

Chemical Name: (Z)-3-(acetoxyimino)-5-chloro-1-(2,5-dichlorobenzyl)indolin-2-one

Smiles: CC(=O)O/N=C1/C2=CC(Cl)=CC=C2N(CC2=CC(Cl)=CC=C2Cl)C/1=O

InChiKey: OPQRFPHLZZPCCH-PGMHBOJBSA-N

InChi: InChI=1S/C17H11Cl3N2O3/c1-9(23)25-21-16-13-7-12(19)3-5-15(13)22(17(16)24)8-10-6-11(18)2-4-14(10)20/h2-7H,8H2,1H3/b21-16-

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 25 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

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.

References:

  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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