2. GPCR/G Protein Epigenetics Cell Cycle/DNA Damage
  3. G Protein-coupled Receptor Kinase (GRK) HDAC
  4. KR-39038

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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KR-39038 Chemical Structure

KR-39038 Chemical Structure

CAS No. : 2770300-35-9

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5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1800 In-stock
50 mg USD 3000 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target

HDAC5

 

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.

KR-39038 Related Antibodies

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)
Cmax (µg/mL) NA 5.2 ± 2.8
Tmax (h) NA 0.7 ± 0.2
t1/2 (h) 0.7 ± 0.04 2.3 ± 2.9
AUC0-∞ (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.
Molecular Weight

475.00

Formula

C24H32ClFN6O
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1053 mL 10.5263 mL 21.0526 mL
5 mM 0.4211 mL 2.1053 mL 4.2105 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
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C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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.

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KR-39038 Related Classifications

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:

KR-390382770300-35-9KR39038KR 39038G Protein-coupled Receptor Kinase (GRK)HDACHistone deacetylasesHypertrophyHeart failureanti-hypertrophiccardioprotectiveneonatal cardiomyocytesorally activeInhibitorinhibitorinhibit

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