LDN-57444

• CAT Number: I004517
• CAS Number: 668467-91-2
• Molecular Formula: C₁₇H₁₁Cl₃N₂O₃
• Molecular Weight: 397.64
• Purity: ≥95%
• Target: DUB
• Solubility: DMSO 16 mg/ml
• Storage: Desiccate at 4°C
• IC50: 0.4 uM(Ki) [1]
• 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-
• InChIKey: OPQRFPHLZZPCCH-PGMHBOJBSA-N
• SMILES: CC(=O)ON=C1C2=C(C=CC(=C2)Cl)N(C1=O)CC3=C(C=CC(=C3)Cl)Cl

LDN-57444 (CAT: I004517) is a potent inhibitor of the deubiquitinating enzyme UCHL1 (ubiquitin carboxyl-terminal hydrolase L1). It acts as a reversible and competitive inhibitor, binding to the active site of UCHL1. By inhibiting UCHL1, LDN-57444 disrupts the deubiquitination process, which plays a crucial role in protein degradation and cellular homeostasis. LDN-57444 has shown efficacy in preclinical studies and is being explored as a potential therapeutic agent for various diseases, including neurodegenerative disorders and cancer, where UCHL1 is involved in disease progression and pathogenesis.

Reference

[1]. Gong B, et al. Ubiquitin hydrolase Uch-L1 rescues beta-amyloid-induced decreases in synaptic function and contextual memory. Cell. 2006 Aug 25;126(4):775-88.
[2]. Tan YY, et al. Endoplasmic reticulum stress contributes to the cell death induced by UCH-L1 inhibitor. Mol Cell Biochem. 2008 Nov;318(1-2):109-15.