KN-62

Catalog No.S7422

KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM.

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KN-62 Chemical Structure

KN-62 Chemical Structure
Molecular Weight: 721.84

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM.
Targets CaMKII [1]
IC50 0.9 μM(Ki)
In vitro KN-62 suppresses the A23187-induced autophosphorylation of Ca2+/CaM kinase in PC12 D cells. [1] KN-62 (10 μM) inhibits carbachol and potassium-stimulated insulin secretion from rat pancreatic islets. [2] KN-62 also inhibits growth of K562 cells and blocks cell cycle progression. [3]
In vivo KN-62 inhibits seizure-induced expression of brain-derived neurotrophic factor mRNA in adult rat brain. [4]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Kinase assay Total kinase activity of CaMKII, determined in a standard 2 min assay (100 μL), contained 35 mM HEPES, 10 mM MgCl2, 1 mM CaCl2, 10 μg of chicken gizzard myosin 20-kD light chain, 0.1 μM calmodulin, and 10 μM [γ-33]ATP at 30 °C. The kinase reaction is halted by adding 1 mL of 10% trichloroacetic acid.

Cell Assay: [3]

Cell lines K562 cells
Concentrations 10 μM
Incubation Time 48 hours
Method For cell growth analysis, K562 cells are plated in a 3-cm dish with 5 mL of culture medium containing various concentration of KN-62. After two days in these condition cell numbers are counted.

Animal Study: [4]

Animal Models Sprague Dawley Rats
Formulation 0.5 mM KN-62/50% DMSO
Dosages 2 pmol
Administration i.c.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Tokumitsu H, et al. J Biol Chem. 1990, 265(8), 4315-4320.

[2] Wenham RM, et al. Biochem Biophys Res Commun. 1992, 189(1), 128-133.

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Chemical Information

Download KN-62 SDF
Molecular Weight (MW) 721.84
Formula

C38H35N5O6S2

CAS No. 127191-97-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (138.53 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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