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Chemical Structure : GK13S
CAS No.:
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).
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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 is bound 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.
| M.Wt | 390.447 | |
| Formula | C21H22N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-1-cyano-N-(1-(4-(pent-4-yn-1-ylcarbamoyl)phenyl)-1H-imidazol-4-yl)pyrrolidine-3-carboxamide |
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1. Grethe C, et al. Nat Commun. 2022 Oct 10;13(1):5950.
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