Cat. No.: HY-143248

KR-39038

1 Cited Publications

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KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC₅₀ of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression of HDAC5 pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research.

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Pureté: 99.68%
CAS No.: 2770300-35-9
Formule: C₂₄H₃₂ClFN₆O
Masse moléculaire:475.00

Stockage:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

KR-39038 Chemical Structure

CAS No.: 2770300-35-9

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

HDAC5

Voir tous les produits spécifiques à Isoform HDAC :

In Vitro

KR-39038 (0-1.0 μM, 24 h) significantly inhibits angiotensin II-induced cellular hypertrophy and HDAC5 phosphorylation in neonatal cardiomyocytes^[1].

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

Western Blot Analysis^[1]

Cell Line:

Primary neonatal cardiomyocytes (isolated from S.D. rats (1-2 days old) using primary myocardial cell isolation kit)
Concentration:

0 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1.0 μM
Incubation Time:

24 h
Result:

Significantly inhibited angiotensin II-induced cellular hypertrophy at a concentration of 0.1 µM and higher concentrations. Decreased angiotensin II-induced HDAC5 phosphorylation at 0.3 µM and higher concentrations.

In Vivo

KR-39038 (0-30 mg/kg, Orally, once daily for 14 days) effectively attenuates both cardiac hypertrophy and dysfunction in experimental heart failure^[1].
Pharmacokinetic Parameters of KR-39038 in Sprague-Dawley rats^[1].

Parameters	IV (5 mg/kg)	PO (300 mg/kg)
C_max (µg/mL)	NA	5.2 ± 2.8
T_max (h)	NA	0.7 ± 0.2
t_1/2 (h)	0.7 ± 0.04	2.3 ± 2.9
AUC_0-∞ (µg*h/mL)	3.4 ± 1.0	8.9 ± 5.0
CL (L/h/kg)	1.6 ± 0.5	NA
Vss (L/kg)	1.2 ± 0.2	NA
F (%)		4.3 ± 2.4

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

Animal Model:

C57BL/6 mice (male, 20-24 g, transverse aortic constriction)^[1]
Dosage:

30 mg/kg
Administration:

Orally, once a day for 2 weeks, starting from 24 h after the operation
Result:

Showed a 43% reduction in the left ventricular weight, and significantly attenuated the development of cardiac hypertrophy.

Animal Model:

Sprague-Dawley (S.D.) rats (male, 380-420 g, coronary artery ligation)^[1]
Dosage:

10 mg/kg, 30 mg/kg
Administration:

Orally, once a day for 12 weeks, starting from 24 h after surgery
Result:

Showed significant preservation of cardiac function and attenuation of myocardial remodeling in a rat model of chronic heart failure following coronary artery ligation.

Animal Model:

Sprague-Dawley (S.D.) rats^[1]
Dosage:

5 mg/kg (IV), 300 mg/kg (Orally)
Administration:

IV or Orally, single (Pharmacokinetic Analysis)
Result:

The AUC_∞ values after intravenous injection with 10 mg/kg and oral administration of 300 mg/kg of KR-39038 were 3.4 ± 1.0 and 8.9 ± 5.0 µg·h/mL, respectively, resulting in 4.3% bioavailability.

Chemical Information

CAS No. 2770300-35-9
Appearance Solid
Masse moléculaire 475.00
Formule C₂₄H₃₂ClFN₆O
Color White to yellow
SMILES

O=C1N=C(C2=C(Cl)C=CC=C2)NC3=CC(NCCCNCCCCNCCCN)=C(C=C13)F
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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

Solvant et solubilité

In Vitro:

DMSO : 115 mg/mL (242.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (210.53 mM; ultrasonic and warming and heat to 80°C)

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

2.1053 mL

10.5263 mL

21.0526 mL

5 mM

0.4211 mL

2.1053 mL

4.2105 mL

10 mM

0.2105 mL

1.0526 mL

2.1053 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Lee JH, et al. KR-39038, a Novel GRK5 Inhibitor, Attenuates Cardiac Hypertrophy and Improves Cardiac Function in Heart Failure. Biomol Ther (Seoul). 2020 Sep 1;28(5):482-489. [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
H₂O / DMSO	1 mM	2.1053 mL	10.5263 mL	21.0526 mL	52.6316 mL
	5 mM	0.4211 mL	2.1053 mL	4.2105 mL	10.5263 mL
	10 mM	0.2105 mL	1.0526 mL	2.1053 mL	5.2632 mL
	15 mM	0.1404 mL	0.7018 mL	1.4035 mL	3.5088 mL
	20 mM	0.1053 mL	0.5263 mL	1.0526 mL	2.6316 mL
	25 mM	0.0842 mL	0.4211 mL	0.8421 mL	2.1053 mL
	30 mM	0.0702 mL	0.3509 mL	0.7018 mL	1.7544 mL
	40 mM	0.0526 mL	0.2632 mL	0.5263 mL	1.3158 mL
	50 mM	0.0421 mL	0.2105 mL	0.4211 mL	1.0526 mL
	60 mM	0.0351 mL	0.1754 mL	0.3509 mL	0.8772 mL
	80 mM	0.0263 mL	0.1316 mL	0.2632 mL	0.6579 mL
	100 mM	0.0211 mL	0.1053 mL	0.2105 mL	0.5263 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

KR-39038

1 Cited Publications

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KR-39038

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Kinase Inhibitor Library

Histone Modification Research Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) KR-39038

Voir tous les produits spécifiques à Isoform HDAC

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

KR-39038

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Kinase Inhibitor Library

Histone Modification Research Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) KR-39038

Voir tous les produits spécifiques à Isoform HDAC

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

KR-39038 Related Classifications

Cat. No.: HY-143248