Home Neuronal Signaling CaMK inhibitor KN-62

KN-62

Catalog No.S7422

For research use only.

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

CAS No. 127191-97-3

Selleck's KN-62 has been cited by 11 Publications

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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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human lymphocytes MlnNSpVv[3Srb36gZZN{[Xl? NUH5Sml3SW62YXfvcol{fCCjY4Tpeol1gSCjdDDQNng4KHKnY3XweI9zKGmwIHj1cYFvKGy7bYDoc4N6fGW|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQWTQMYlv\HWlZXSgRoEzMyCrbn\seZgtKEmFNUC9NVIvPTlibl2= NVP6fGlGOTlzOUG1PFU>
HEK293 cells M2\p[GZ2dmO2aX;uJIF{e2G7 MnTLRY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBROlh5IILlZ4VxfG:{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCEelHUVE1qdmS3Y3XkJINidGOrdX2gbY5ndHW6LDDJR|UxRTVyLkGyJI5O NUnqeoJEOTlzOUG1PFU>
THP1 cells M2rrUGZ2dmO2aX;uJIF{e2G7 MWrJcohq[mm2aX;uJI9nKEK8LVHUVE1qdmS3Y3XkJGlNOS2kZYThJJJmdGWjc3WgbY4hVFCVL1nGUk1o[W2vYT3kbYZn\XKnboTpZZRm\CCqdX3hckBVUFBzIHPlcIx{KGK7IFXMTXNCNCCLQ{WwQVAvODhzIN88US=> MorvNVkyOTB2MkC=
Click to View More Cell Line Experimental Data
In vivo KN-62 inhibits seizure-induced expression of brain-derived neurotrophic factor mRNA in adult rat brain. [4]

Protocol (from 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 Research:

[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 Research:

[4]
  • Animal Models: Sprague Dawley Rats
  • Dosages: 2 pmol
  • Administration: i.c.v.

Solubility (25°C)

In vitro

 DMSO 100 mg/mL
(138.53 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 721.84
Formula

C38H35N5O6S2
CAS No. 127191-97-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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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.

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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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