LDN-57444
Synonym(s):3-(O-acetyloxime), 5-chloro-1-[(2,5-dichlorophenyl)methyl]-1H-Indole-2,3-dione;C30;LDN 57444;LDN-57444, Ubiquitin C-Terminal Hydrolase L1 Inhibitor, Ubiquitin C-Terminal Esterase L1 Inhibitor, Ubiquitin Thiolesterase L1 Inhibitor;UCH-L1 Inhibitor - CAS 668467-91-2 - Calbiochem
- CAS NO.:668467-91-2
- Empirical Formula: C17H11Cl3N2O3
- Molecular Weight: 397.64
- MDL number: MFCD09037562
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-05-18 11:31:10
What is LDN-57444?
Description
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, Ki = 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.
The Uses of LDN-57444
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.
What are the applications of Application
UCH-L1 Inhibitor is a potent, reversible, active site-directed UCH-L1 inhibitor
Biochem/physiol Actions
LDN-57444 is a potent, reversible, competitive and active site-directed inhibitor of UCHL1
References
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
Properties of LDN-57444
Boiling point: | 534.4±60.0 °C(Predicted) |
Density | 1.50±0.1 g/cm3(Predicted) |
storage temp. | 2-8°C |
solubility | DMSO: soluble16mg/mL |
form | solid |
pka | -2.57±0.20(Predicted) |
color | Yellow |
Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 week. |
Safety information for LDN-57444
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for LDN-57444
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