Home Neuronal Signaling CaMK inhibitor KN-62 For research use only.

KN-62

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 KN-62 for CaMK V is 0.8 μM.

KN-62 Chemical Structure

KN-62 Chemical Structure

CAS No. 127191-97-3

Purity & Quality Control

KN-62 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human lymphocytes Function assay Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced Ba2+ influx, IC50=12.59 nM 19191585
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 19191585
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 19110420
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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; 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 KN-62 for CaMK V is 0.8 μM.
Targets
CaMKⅠ [5] CaMKⅣ [6] P2RX7 [8] CaMKⅤ [7] CaMKII [1]
0.8 μM(Ki) 0.9 μM(Ki)
In vitro
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]
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.
Cell Research 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.
In Vivo
In vivo KN-62 inhibits seizure-induced expression of brain-derived neurotrophic factor mRNA in adult rat brain. [4]
Animal Research Animal Models Sprague Dawley Rats
Dosages 2 pmol
Administration i.c.v.

Chemical Information & Solubility

Molecular Weight 721.84 Formula

C38H35N5O6S2
CAS No. 127191-97-3 SDF Download KN-62 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (138.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

Handling Instructions

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