Cat. No.: HY-156863

GRK2 Inhibitor 2

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

GRK2 Inhibitor 2 is an orally active and selective G protein-coupled receptor kinase 2 (GRK) inhibitor with an IC₅₀ of 19 nM. GRK2 Inhibitor 2 also inhibits Aurora-A with an IC₅₀ of 137 nM. GRK2 Inhibitor 2 can be used in the study of congestive heart failure (HF).

For research use only. We do not sell to patients.

Purity: 99.92%
CAS No.: 2592436-21-8
Formula: C₁₉H₁₆N₄O₂
Molecular Weight:332.36

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

GRK2 Inhibitor 2 Chemical Structure

CAS No.: 2592436-21-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

GRK2	Aurora A 137 nM (IC₅₀)

All Aurora Kinase Isoforms :

In Vitro

GRK2 Inhibitor 2 (Compound 8h) (1-10 μM; 8 h) increases β-AR mediated cAMP accumulation in HEK293 cells overexpressed with GRK2^[1].
GRK2 Inhibitor 2 (Compound 8h) (0.1-10 μM; 8 h) increases the calcium transient beat rate in human stem cell-derived cardiomyocyte treated with isoproterenol (HY-B1670) and effectively regulates cardiomyocyte function^[1].

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

In Vivo

Pharmacokinetic Analysis in C57BL Mice^[1]

Dose i.v./p.o. (mg/kg)	CL_p (mL/min/kg)	Vd_ss (L/kg)	i.v. t_1/2 (h)	p.o. t_1/2 (h)	C_max (μM)	t_max (h)	Oral AUC (μM.h.kg)	F (%)
2/10	29.1	2.01	1.01	2.41	4.96	0.83	11.89	65.3

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

Chemical Information

CAS No. 2592436-21-8
Appearance Solid
Molecular Weight 332.36
Formula C₁₉H₁₆N₄O₂
Color White to off-white
SMILES

O=C1C2=C(C=NN1CC3=CC(OC)=CC=C3)C=CC(C4=CNN=C4)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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Journal Impact Factor

Commun Biol

Cell-based and isoform-selective G protein-coupled receptor kinase assays for comprehensive inhibitor evaluation. [Abstract]

2026 Jan 16;9(1):287. PMID: 41545717

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (300.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0088 mL

15.0439 mL

30.0879 mL

5 mM

0.6018 mL

3.0088 mL

6.0176 mL

10 mM

0.3009 mL

1.5044 mL

3.0088 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Handling Instructions (2659 KB)

References

[1]. Xu G, et al. Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor. Bioorg Med Chem Lett. 2020 Dec 1;30(23):127602. [Content Brief]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0088 mL	15.0439 mL	30.0879 mL	75.2196 mL
	5 mM	0.6018 mL	3.0088 mL	6.0176 mL	15.0439 mL
	10 mM	0.3009 mL	1.5044 mL	3.0088 mL	7.5220 mL
	15 mM	0.2006 mL	1.0029 mL	2.0059 mL	5.0146 mL
	20 mM	0.1504 mL	0.7522 mL	1.5044 mL	3.7610 mL
	25 mM	0.1204 mL	0.6018 mL	1.2035 mL	3.0088 mL
	30 mM	0.1003 mL	0.5015 mL	1.0029 mL	2.5073 mL
	40 mM	0.0752 mL	0.3761 mL	0.7522 mL	1.8805 mL
	50 mM	0.0602 mL	0.3009 mL	0.6018 mL	1.5044 mL
	60 mM	0.0501 mL	0.2507 mL	0.5015 mL	1.2537 mL
	80 mM	0.0376 mL	0.1880 mL	0.3761 mL	0.9402 mL
	100 mM	0.0301 mL	0.1504 mL	0.3009 mL	0.7522 mL

Keywords

GRK2 Inhibitor 2

1 Cited Publications

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GRK2 Inhibitor 2

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Publications Citing Use of MedChemExpress (MCE) GRK2 Inhibitor 2

All Aurora Kinase Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GRK2 Inhibitor 2

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Kinase Inhibitor Library

Autophagy Compound Library

Anti-Aging Compound Library

Anti-Cardiovascular Disease Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) GRK2 Inhibitor 2

All Aurora Kinase Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GRK2 Inhibitor 2 Related Classifications

HY-156863 Related Classifications