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KN-92 phosphate

Catalog No.
A3531
CaMKII inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$300.00
In stock
5mg
$246.00
In stock
10mg
$339.00
In stock
50mg
$986.00
Ship with 10-15 days
200mg
$2,262.00
Ship with 10-15 days

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Background

KN-92 is the inactive analog of Ca2+/calmodulin-dependent kinase II (CaMKII) inhibitor KN-93. KN-92 has been often used as negative control for KN-93.KN-92 significantly reduced the sustained current amplitudes at the end of the 5-s depolarizing pulses of a wide range of Kv channels such as Kv1.5 and Kv1.2 [1].

Reference:
[1]. Rezazadeh S, Claydon TW, Fedida D.KN-93(2-[N-(2-hydroxyethyl)]-N-(4-methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine), a calcium/calmodulin-dependent protein kinase II inhibitor, is a direct extracellular blocker of voltage-gated potassium channels.J PharmacolExpTher. 2006 Apr;317(1):292-9.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt554.98
Cas No.1135280-28-2
FormulaC24H28ClN2O7PS
SynonymsKN 92 phosphate;KN92 phosphate
Solubility≥25 mg/mL in DMSO, ≥43.1 mg/mL in EtOH with gentle warming,insoluble in H2O
Chemical Name(E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-4-methoxybenzenesulfonamide phosphate
SDFDownload SDF
Canonical SMILESCN(CC1=CC=CC=C1NS(C2=CC=C(OC)C=C2)(=O)=O)C/C([H])=C([H])/C3=CC=C(Cl)C=C3.OP(O)(O)=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

rabbit hypertrophic cardiac myocytes

Preparation method

The solubility of this compound in DMSO is >25mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.5 μmol/L and 1 μmol/L

Applications

KN-92 is the inactive analog of KN-93. Under the conditions of low potassium, low magnesium Tyrode’s solution perfusion, and slow frequency electrical stimulation, the incidence of early after-depolarizations (EADs) was 0/12, 11/12, 10/12, and 5/12 in sham group, left ventricular hypertrophy (LVH) group, KN-92 group (0.5 μmol/L), and KN-93 group (0.5 μmol/L), respectively. When the drug concentration was increased to 1 μmol/L in KN-92 group and KN-93 group, the incidence of EADs was 10/12 and 2/12, respectively. When the drug concentration was 0.5 μmol/L in KN-92 and KN-93 groups, the peak ICa, L at 0 mV was decreased by (9.4±2.8)% and (10.5±3.0)%, respectively. When the drug concentration was increased to 1 μmol/L, the peak ICa, L values were lowered by (13.4±3.7)% and (40±4.9)%, respectively.

Animal experiment [2]:

Animal models

Spontaneously hypertensive rats

Dosage form

1 μmol/L

Application

In spontaneously hypertensive rats, action potential duration alternans (APD-ALT) was evoked at significantly lower pacing rate, KN-93 (1 μmol/L), but not its inactive analog, KN-92 (1 μmol/L), completely reversed these changes in APD-ALT. The magnitude of APD-ALT was also significantly greater in SHR than WKY and was completely normalized by KN-93. KN-93 also abolished ventricular fibrillation (VF) induced by rapid pacing in SHR.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Ke J1, Chen F, Zhang C, et al. Effects of calmodulin-dependent protein kinase II inhibitor, KN-93, on electrophysiological features of rabbit hypertrophic cardiac myocytes. J Huazhong Univ Sci Technolog Med Sci. 2012 Aug;32(4):485-9.

[2]. Mitsuyama H1, Yokoshiki H2, Watanabe M1, et al. Ca2+/calmodulin-dependent protein kinase II increases the susceptibility to the arrhythmogenic action potential alternans in spontaneously hypertensive rats. Am J Physiol Heart Circ Physiol. 2014 Jul 15;307(2):H199-206.

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