Catalog No.: PC-49371Not For Human Use, Lab Use Only.
GK13S is a highly potent, specific and covalent inhibitor of deubiquitinase UCHL1 with IC50 of 87 nM, displays exquisite specificity for UCHL1 over the other UCH family members (IC50>10 uM).
GK13S is a highly potent, specific and covalent inhibitor of deubiquitinase UCHL1 with IC50 of 87 nM, displays exquisite specificity for UCHL1 over the other UCH family members (IC50>10 uM).
GK13S inhibits recombinant UCHL1 (0.8 uM) with IC50 of 50 nM in a Ubiquitin rhodamine cleavage assay.
Inhibition of UCHL1 by GK13S does not impair cell growth in HEK293 cells.
GK13S reduces monoubiquitin in U-87 MG cells and thereby phenocopies the effect of a UCHL1 mutant mouse.
GK13S binds covalently to the catalytic cysteine Cys90 through an isothiourea with its cyanamide warhead and occupies a shallow cleft that, during catalysis, guides the Ubiquitin C-terminal LRGG peptide to the active site.
