LDN-57444

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

LDN-57444 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  The ubiquitin C-terminal hydrolase L1 (UCH-L1) is a member of a family of de-ubiquitinating enzymes that can generate free ubiquitin from ubiquitin precursors via its ubiquitin ligase activity. By associating with free ubiquitin, it also prevents its degradation. Neuronal UCH-L1 has been linked to Parkinson’s disease, the development of tumors, and neuropathic pain. LDN-57444 is an inhibitor of UCH-L1 activity (IC₅₀ = 0.88, K_i = 0.4 μM) that demonstrates selectivity for UCH-L1 compared to UCH-L3 (IC₅₀ = 25 μM). Loss of UCH-L1 activity causes cell death through the apoptosis pathway due to an impaired ubiquitin-proteasome pathway. LDN-57444-induced reduction of free ubiquitin has been shown to create dramatic alterations in synaptic structure and function, increasing spine size while decreasing spine density in hippocampal neurons.

• Verwenden

  LDN 57444 is an inhibitor of UCH-L1, an enzyme expressed by certain lung tumor-derived cell lines, suggesting that this enzyme plays a role in tumor progression.

• Biochem/physiol Actions

  LDN-57444 is a potent, reversible, competitive and active site-directed inhibitor of UCHL1

• Einzelnachweise

  1) Liu et al. (2003), Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line; Chem. Biol., 10 837 2) Tan et al. (2008), Endoplasmic reticulum stress contributes to the cell death induced by UCH-L1 inhibitor; Mol. Cell. Biochem., 318 109 3) Cartier et al. (2009), Regulation of synaptic structure by ubiquitin C-terminal hydrolase L1; J. Neurosci., 29 7857

LDN-57444 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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