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KN-62 CaMK inhibitor

Name: KN-62
Brand: Selleck Chemicals
SKU: S7422
Availability: InStock
Rating: 5 (21 reviews)

Cat.No.S7422

KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM; also a non-competitive antagonist of the purinergic receptor P2RX7 (IC50 = 15 nM). It is selective for CaMKII relative to PKA, PKC and MLCK, but inhibits CaMKI and CaMKIV equally well, The Ki value of this compound for CaMK V is 0.8 μM.

Chemical Structure

Molecular Weight: 721.84

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Quality Control

Batch: Purity: 99.89%

99.89

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other CaMK Inhibitors	KN-93 Phosphate KN-93 STO-609 KN-92 phosphate NH125 KN-93 hydrochloride

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
human lymphocytes	Function assay	Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced Ba2+ influx, IC50=12.59 nM
HEK293 cells	Function assay	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium influx, IC50=50.12 nM
THP1 cells	Function assay	Inhibition of Bz-ATP-induced IL1-beta release in LPS/IFN-gamma-differentiated human THP1 cells by ELISA, IC50=0.081 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (138.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (1.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.830mg/ml (1.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	721.84	Formula	C₃₈H₃₅N₅O₆S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	127191-97-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN(C(CC1=CC=C(C=C1)OS(=O)(=O)C2=CC=CC3=C2C=CN=C3)C(=O)N4CCN(CC4)C5=CC=CC=C5)S(=O)(=O)C6=CC=CC7=C6C=CN=C7

Mechanism of Action

Targets/IC₅₀/Ki	CaMKⅠ CaMKⅣ P2RX7 CaMKⅤ 0.8 μM(Ki) CaMKII 0.9 μM(Ki)
In vitro	KN-62 suppresses the A23187-induced autophosphorylation of Ca2+/CaM kinase in PC12 D cells. This compound (10 μM) inhibits carbachol and potassium-stimulated insulin secretion from rat pancreatic islets. It also inhibits growth of K562 cells and blocks cell cycle progression.
Kinase Assay	Kinase assay
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.
In vivo	KN-62 inhibits seizure-induced expression of brain-derived neurotrophic factor mRNA in adult rat brain.
References	[1] https://pubmed.ncbi.nlm.nih.gov/2155222/ [2] https://pubmed.ncbi.nlm.nih.gov/1333187/ [3] https://pubmed.ncbi.nlm.nih.gov/8123019/ [4] https://pubmed.ncbi.nlm.nih.gov/9753146/ [5] https://pubmed.ncbi.nlm.nih.gov/24600394/ [6] https://pubmed.ncbi.nlm.nih.gov/8195196/ [7] https://pubmed.ncbi.nlm.nih.gov/8386178/ [8] https://pubmed.ncbi.nlm.nih.gov/9720806/

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Handling Instructions

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