GRK5-IN-3

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Fiche technique Instruction de manipulation

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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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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

Masse moléculaire
443.46

Formule
C₂₃H₂₁N₇O₃

CAS No.
2410793-22-3

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

Fiche technique (277 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]

[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.

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GRK5-IN-3 Related Classifications

GPCR/G Protein

G Protein-coupled Receptor Kinase (GRK)

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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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Size		Stock
MOQ		Minimum order quantity
50 mg		Obtenir un devis
100 mg		Obtenir un devis
250 mg		Obtenir un devis
Other size		Obtenir un devis

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
Masse moléculaire	443.46
Formule	C₂₃H₂₁N₇O₃
CAS No.	2410793-22-3
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	Fiche technique (277 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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GRK5-IN-3

GRK5-IN-3 Related Antibodies

Recommandations en vedette

•Related Small Molecules:

•Related Proteins:

Activité biologique

Pureté et documentation

Références

Avis client

GRK5-IN-3 Related Antibodies

GRK5-IN-3 Related Classifications

Calculateur de molarité

Calculateur de dilution

The molarity calculator equation

The dilution calculator equation

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