KN-93 Phosphate

Catalog No.S7423

For research use only.

KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy.

KN-93 Phosphate Chemical Structure

CAS No. 1188890-41-6

Selleck's KN-93 Phosphate has been cited by 41 publications

Purity & Quality Control

Choose Selective CaMK Inhibitors

Biological Activity

Description KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy.
Targets
CaMKII [1]
(Cell-free assay)
0.37 μM(Ki)
In vitro

KN-93 inhibits dopamine formation in PC12h cells by modulating the reaction rate of TH to reduce the Ca(2+)-mediated phosphorylation levels of the TH molecule. [1] KN-93 inhibits serum-induced fibroblast cell growth with IC50 of 8 μM, and induces apoptosis after prolonged G1 arrest. [2] KN-93 inhibits androgen receptor activity and p53-independently induces cell death in PCa cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells NYH5WJBZTnWwY4Tpc44h[XO|YYm= MkDhNlAhdWmwcx?= NVjwR2h[UW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBESU2NMjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KGGodHXyJFIxKG2rboOsJGlEPTB;MT62{txO MmGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{OUK0PFIoRjJzMkmyOFgzRC:jPh?=
Assay
Methods Test Index PMID
Western blot p-CDK2 ; p-CDK9 / CDK9 21448926
In vivo KN-93 (5 μg) ameliorates levodopa-induced dyskinesia by lowering the expression of pGluR1S845 in a rat model of Parkinson’s disease. [4] In MRL/lpr Foxp3-GFP mice, KN-93 results in a significant induction of Treg cells in the spleen, peripheral lymph nodes and peripheral blood, and decreases skin and kidney damage. [5]

Protocol (from reference)

Kinase Assay:[1]
  • Measurement of activities of autophosphorylated/non-autophosphorylate CaMKII:

    CaMKII activity is measured utilizing syntideII as a substrate. Purified CaMKII is pre-incubated in the assay mixture ( 35 mM Hepes-Na ( pH 8.0 ), 10 mM MgC12, 0.5 μM CaM, 5 μM ATP, 1 mM CaCl2 or 1 mM EGTA, total 25 μL) at 30 °C for 2 minutes. After this pre-incubation, the protein substrate/radioactive ATP mixture is added to the same test tube and the preparation is further incubated at 30 °C, for 5 minutes ( final assay condition; 35 mM Hepes-Na (pH 8.0), 10 mM MgCl2, 0.125 μM CaCl2, 20 μM syntideII, 11.25 μM [ γ-32P] ATP, 10 % DMSO and indicated concentrations of KN-93, supplemented with 0.25 mM CaCl2 and 2 mM EGTA (for autophosphorylated samples) or 0.25 mM EGTA and 2 mM CaCl2 (for nonautophosphorylated samples ), total 100 μL ). The reaction is terminated by adding of 25 μL of 100 % ( w/v ) ice-cold TCA. After centrifugation, 80 μL of the supernatant is applied to phosphocellulose paper. The filters are then washed with 75 mM H3P04 for 15 min with continuous agitation. After 4-cycles of washing, the radioactivity retains on the filter paper is quantified in a liquid scintillation counter.

Cell Research:[2]
  • Cell lines: NIH 3T3 fibroblasts
  • Concentrations: ~24 μM
  • Incubation Time: 70 hours
  • Method: NIH 3T3 fibroblasts are cultured on polystyrene dishes in DMEM and fetal bovine serum, supplemented with penicillin/streptomycmn in a 5% CO2 humidified chamber at 37 癈. Cell growth is measured by using the MTT dye reduction method.
Animal Research:[4]
  • Animal Models: Sprague Dawley female rats
  • Dosages: ~5 μg
  • Administration: Intrastriatal administration

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 599.03
Formula

C26 H29 Cl N2 O4 S . H3 O4 P

CAS No. 1188890-41-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(CC=CC1=CC=C(C=C1)Cl)CC2=CC=CC=C2N(CCO)S(=O)(=O)C3=CC=C(C=C3)OC.OP(=O)(O)O

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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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