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KN-93 Phosphate CaMK inhibitor

Name: KN-93 Phosphate
Brand: Selleck Chemicals
SKU: S7423
Availability: InStock
Rating: 5 (51 reviews)

Cat.No.S7423

KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with K_i of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy.This product is not soluble in saline. Please do not dissolve it in saline for administration.

Chemical Structure

Molecular Weight: 599.03

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Quality Control

Batch: Purity: 99.35%

99.35

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other CaMK Products	KN-93 KN-62 STO-609 KN-92 phosphate NH125 KN-93 hydrochloride CaMKII (pan) Antibody [G5E11] CaMKIIβ Antibody [C10N23] Calmodulin 1/2/3-C-terminal Antibody [E5K8] CaMKII-α Antibody [F14D18]

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Sf9 cells	Function assay		20 mins		Inhibition of recombinant CAMK2 expressed in Sf9 cells after 20 mins, IC50=1.6μM	21292482
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (166.93 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

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	1%DMSO 1 10%PEG300 2 89%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.09mM)	Taking the 1 mL working solution as an example, add 10 μL of 125 mg/ml clarified DMSO stock solution to 100 μL of PEG300, mix evenly to clarify it; then continue to add 890 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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.

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	599.03	Formula	C₂₆ H₂₉ Cl N₂ O₄ S . H₃ O₄ P	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1188890-41-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	CaMKII (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. KN-93 inhibits serum-induced fibroblast cell growth with IC50 of 8 μM, and induces apoptosis after prolonged G1 arrest. KN-93 inhibits androgen receptor activity and p53-independently induces cell death in PCa cells.
Kinase Assay	Measurement of activities of autophosphorylated/non-autophosphorylate CaMKII
Kinase Assay	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.
In vivo	KN-93 (5 μg) ameliorates levodopa-induced dyskinesia by lowering the expression of pGluR1S845 in a rat model of Parkinson’s disease. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/1662507/ [2] https://pubmed.ncbi.nlm.nih.gov/8519682/ [3] https://pubmed.ncbi.nlm.nih.gov/20023417/ [4] https://pubmed.ncbi.nlm.nih.gov/23983471/ [5] https://pubmed.ncbi.nlm.nih.gov/24829059/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-CDK2 p-CDK9 / CDK9		21448926

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Handling Instructions

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