LDN-57444

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.Formal Name: 5-chloro-1-[(2,5-dichlorophenyl)methyl]-1H-indole-2,3-dione 3-(O-acetyloxime). CAS Number: 668467-91-2. Synonyms: Ubiquitin C-terminal Hydrolase L1 Inhibitor, UCH-L1 Inhibitor. Molecular Formula: C17H11Cl3N2O3. Formula Weight: 397.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMF:PBS(pH7.2) (1:2): 0.3 mg/ml, DMSO: 3 mg/ml. lambdamax: 226, 254 nm. SMILES: O=C1N(CC2=C(Cl)C=CC(Cl)=C2)C3=CC=C(Cl)C=C3/C1=N/OC(C)=O. InChi Code: 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-. InChi Key: OPQRFPHLZZPCCH-PGMHBOJBSA-N.