Biological Activity
IMP-1710 is an inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1; IC50 = 38 nM in a fluorescence polarization assay) that contains an alkyne moiety for use in click chemistry reactions.1 It is selective for UCH-L1 over a panel of 20 deubiquitinating enzymes at 1 μM. IMP-1710 inhibits TGF-β1-induced fibroblast-to-myofibroblast transition (FMT) in primary lung fibroblasts isolated from patients with idiopathic pulmonary fibrosis (IC50 = 740 nM). It has been used for labeling UCH-L1 in cell-based assays, followed by click reactions with azide-modified TAMRA and biotin capture reagents.
References
1.Panyain, N., Godinat, A., Lanyon-Hogg, T., et al.Discovery of a potent and selective covalent inhibitor and activity-based probe for the deubiquitylating enzyme UCHL1, with antifibrotic activityJ. Am. Chem. Soc.142(28)12020-12026(2020)
