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GK13S

Chemical Structure : GK13S

CAS No.:

GK13S (UCHL1 inhibitor GK13S)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 390.447
Formula C21H22N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-1-cyano-N-(1-(4-(pent-4-yn-1-ylcarbamoyl)phenyl)-1H-imidazol-4-yl)pyrrolidine-3-carboxamide

References

1. Grethe C, et al. Nat Commun. 2022 Oct 10;13(1):5950.

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