KN-62

Catalog No.S7422

KN-62 Chemical Structure

Molecular Weight(MW): 721.84

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.

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Choose Selective CaMK Inhibitors

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 M{HCWWZ2dmO2aX;uJIF{e2G7 NHe3UJBCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IGCyXFchemWlZYD0c5IhcW5iaIXtZY4hdHmvcHjvZ5l1\XNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDVGCtbY5lfWOnZDDCZVIsKGmwZnz1fEwhUUN3ME2xNk42QSCwTR?= NUnvU2ZGOTlzOUG1PFU>
HEK293 cells NVmwdFB3TnWwY4Tpc44h[XO|YYm= MXjBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHAzYDdicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEK8QWTQMYlv\HWlZXSgZ4Ft[2m3bTDpcoZtfXhuIFnDOVA:PTBwMUKgcm0> M4KxfVE6OTlzNUi1
THP1 cells NEG1TJFHfW6ldHnvckBie3OjeR?= NXKyNnBrUW6qaXLpeIlwdiCxZjDCfk1CXFBvaX7keYNm\CCLTEGtZoV1[SC{ZXzlZZNmKGmwIFzQV{9KTk5vZ3HtcYEu\GmoZnXy[Y51cWG2ZXSgbJVu[W5iVFjQNUBk\WyuczDifUBGVEmVQTygTWM2OD1yLkC4NUDPxE1? NIHiNIQyQTFzMESyNC=>

... 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

Kinase Assay:

[1]

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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]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[4]

+ Expand
  • Animal Models: Sprague Dawley Rats
  • Formulation: 0.5 mM KN-62/50% DMSO
  • Dosages: 2 pmol
  • Administration: i.c.v.
    (Only for Reference)

Solubility (25°C)

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

Molecular Weight 721.84
Formula

C38H35N5O6S2

CAS No. 127191-97-3
Storage powder
Synonyms N/A

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID