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Cat. No.: HY-150021

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GRK5-IN-3

Name: GRK5-IN-3
Brand: MedChemExpress
SKU: HY-150021
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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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CAS No.: 2410793-22-3

Formule: C₂₃H₂₁N₇O₃

Masse moléculaire:443.46

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

GRK5-IN-3 Chemical Structure

CAS No.: 2410793-22-3

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Data Download

Data Sheet (277 KB)

Instruction de manipulation (2659 KB)

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Activité biologique

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.

Chemical Information

CAS No. 2410793-22-3

Masse moléculaire 443.46

Formule C₂₃H₂₁N₇O₃

SMILES

O=C(NC1=CC=C(C(OC)=C1)NC2=NC(NC3=C(C(N)=O)C=CC=C3)=C4C=CNC4=N2)C=C

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)

COA (2659 KB)

Elemental Analysis Report (2659 KB)

HNMR (2659 KB)

CNMR (2659 KB)

RP-HPLC (2659 KB)

NP-HPLC (2659 KB)

MS (2659 KB)

LCMS (2659 KB)

IR (2659 KB)

GC (2659 KB)

OR (2659 KB)

SDS-PAGE (2659 KB)

SEC-HPLC (2659 KB)

Other Report (2659 KB)

Instruction de manipulation (2659 KB)

Références

[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

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

GRK5-IN-3 Related Classifications

HY-150021 Related Classifications

GPCR/G Protein

G Protein-coupled Receptor Kinase (GRK)

Aires thérapeutique

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Keywords

GRK5-IN-3
2410793-22-3
G Protein-coupled Receptor Kinase (GRK)
pyrrolopyrimidine
cancer
neurodegeneration
type 2 diabetes
CVD
cardiovascular disease
heart failure
G protein-coupled receptor kinase 5
Inhibitor
inhibitor
inhibit

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GRK5-IN-3

Activité biologique

Description

IC50 & Target

In Vitro

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

GRK5-IN-3 Related Classifications

HY-150021 Related Classifications

Bioz

Keywords

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