2. GPCR/G Protein
  3. G Protein-coupled Receptor Kinase (GRK)
  4. GRK5-IN-3

GRK5-IN-3 is a covalent inhibitor of GRK5 (G Protein-Coupled Receptor Kinase 5). GRK5-IN-3 shows potent inhibitory effect to GRK5 and GRK6 with IC50s of 0.22 μM and 0.41 μM, respectively.

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GRK5-IN-3 Chemical Structure

GRK5-IN-3 Chemical Structure

CAS No. : 2410793-22-3

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GRK5-IN-3 Related Antibodies

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Description

GRK5-IN-3 is a covalent inhibitor of GRK5 (G Protein-Coupled Receptor Kinase 5). GRK5-IN-3 shows potent inhibitory effect to GRK5 and GRK6 with IC50s of 0.22 μM and 0.41 μM, respectively[1].

IC50 & Target

IC50: 0.22 μM (GRK5), 0.41 μM (GRK6)[1]
In Vitro

GRK5 can be used to cancer, neurodegeneration, type 2 diabetes, heart failure and cardiovascular (CVD) research[1].
GRK5-IN-3 (Compound 5) (0-333 μM; 0-4 h) inhibits GRK5 in a time-dependent manner with IC50s of 59 μM (0 h), 11.3 μM (0.5 h), 6.2 μM (1 h), and 0.22 μM (4 h), respectively[1].
GRK5-IN-3 (0-333 μM; 0-4 h) also shows selectivity to human GRK5 over bovine GRK2 and bovine GRK1, with IC50s >100 μM (GRK1/2), respectively[1].
GRK5-IN-3 (0-333 μM; 0-4 h) exerts inhibition against GRK5, while light activated ROS as substrate, with IC50s of >100 μM (0 h), 4.2 μM (0.5 h), 3.4 μM (1 h), and 0.9 μM (4 h), respectively[1].
GRK5-IN-3 (0-333 μM; 4 h) shows no inhibitory effect on mutant GRK5 (GRK5-C474S, Cys474 mutated to serine), with IC50 values >100 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GRK5-IN-3 Related Antibodies
Molecular Weight

443.46

Formula

C23H21N7O3
CAS No.
SMILES

O=C(NC1=CC=C(C(OC)=C1)NC2=NC(NC3=C(C(N)=O)C=CC=C3)=C4C=CNC4=N2)C=C
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GRK5-IN-3 Related Classifications

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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-32410793-22-3G Protein-coupled Receptor Kinase (GRK)pyrrolopyrimidinecancerneurodegenerationtype 2 diabetesCVDcardiovascular diseaseheart failureG protein-coupled receptor kinase 5Inhibitorinhibitorinhibit

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