GRK5-IN-4 (Synonyms: CCG-265328)

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GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC₅₀ of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research. GRK5-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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GRK5-IN-4 Chemical Structure

CAS No. : 2410794-89-5

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Description	GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC₅₀ of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research^[1]. GRK5-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
IC₅₀ & Target	IC50: 1.1 ± 0.4 μM (GRK5), 1.8 ± 2 μM (GRK6), >100 μM (GRK2)^[1]
In Vitro	GRK5-IN-4 (Compound 16d) (0-4 h) displays a marked increase in apparent potency as a function of time^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. GRK5-IN-4 Related Antibodies
Molecular Weight	483.52
Formula	C₂₆H₂₅N₇O₃
CAS No.	2410794-89-5
SMILES	O=C(NCC1=CC=C(C(OC)=C1)NC2=NC(NC3=C(C(NC)=O)C=CC=C3)=C4C=CNC4=N2)C#CC
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (270 KB) Handling Instructions (2659 KB)
References	[1]. Rowlands RA, et al. Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. ACS Med Chem Lett. 2019 Nov 12;10(12):1628-1634. [Content Brief]

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GRK5-IN-42410794-89-5CCG-265328CCG265328CCG 265328G Protein-coupled Receptor Kinase (GRK)Pyrrolopyrimidinecovalent inhibitorkinase inhibitorGPCR kinaseheart failureInhibitorinhibitorinhibit

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GRK5-IN-4 (Synonyms: CCG-265328)

GRK5-IN-4 Related Antibodies

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