GRL018-21 | GRK5 inhibitor | Probechem Biochemicals

Chemical Structure : GRL018-21

GRL018-21 (GRL 018-21)

Catalog No.: PC-21461Not For Human Use, Lab Use Only.

GRL018-21 is a highly selective, potent, and non-covalent GRK5 inhibitor with IC50 of 10 nM, >100,000-fold selectivity over GRK2.

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Biological Activity

GRL018-21 is a highly selective, potent, and non-covalent GRK5 inhibitor with IC50 of 10 nM, >100,000-fold selectivity over GRK2.
GRL018-21 forms a hemithioketal intermediate with active site Cys474 in the GRK5 active site.

Physicochemical Properties

M.Wt	526.52
Formula	C29H23FN4O5
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	(R,Z)-N-(1-(4-fluorophenyl)ethyl)-3-((4-(2-(furan-2-yl)-2-oxoacetamido)-3-methyl-1H-pyrrol-2-yl)methylene)-2-oxoindoline-5-carboxamide

References

1. Yueyi Chen, et al. Eur J Med Chem. 2023 Nov 10:264:115931.

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GRL018-21 (GRL 018-21)

Biological Activity

Physicochemical Properties

References

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