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KN-92 hydrochloride

Catalog No.
A3530
Inactive derivative of KN-93,control compound
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$265.00
In stock
5mg
$246.00
In stock
10mg
$339.00
In stock
50mg
$986.00
In stock
200mg
$2,262.00
In stock

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Background

KN-92 is an inactive analog of KN-93. KN-93 is the CaM kinase II inhibitor. [1]

Hearts were treated with the CaM kinase inhibitor KN-93 or the inactive analog KN-92 (0.5 μM) for 10 min before clofilium exposure. Early afterdepolarizations (EADs) were largely inhibited by KN-93 contrasted to KN-92. There were little differences in parameters favoring EADs such as monophasic action potential duration or heart rate in KN-92- or KN-93- treated hearts. CaM kinase activity in situ increased 37% in hearts with EADs compared to hearts without EADs. This increase in CaM kinase activity was prevented by pretreatment with KN-93. [1]

In vitro, KN-93 potently suppressed rabbit myocardial CaM kinase activity (calculated Ki ≤ 2.58 μM), but the inactive analog KN-92 did not (Ki > 100 μM). The actions of KN-93 and KN-92 on ICa and other repolarizing K+currents did not illustrate preferential EAD suppression by KN-93. [1]

Reference:
1.  KN-93, an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase, decreases early afterdepolarizations in rabbit heart. J Pharmacol Exp Ther. 1998 Dec;287(3):996-1006.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt493.45
Cas No.1431698-47-3
FormulaC24H26Cl2N2O3S
SynonymsKN 92 hydrochloride;KN92 hydrochloride
Solubility≥24.65 mg/mL in DMSO, ≥11.73 mg/mL in EtOH with ultrasonic and warming,insoluble in H2O
Chemical Name(E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-4-methoxybenzenesulfonamide hydrochloride
SDFDownload SDF
Canonical SMILESClC1=CC=C(/C=C/CN(C)CC2=CC=CC=C2NS(C3=CC=C(OC)C=C3)(=O)=O)C=C1.Cl
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

NIH 3T3 fibroblasts

Preparation method

The solubility of this compound in DMSO is > 10 mM. 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

72 h, 4-24 μM

Applications

KN-92 is an inactive derivative of KN-93. KN-92 is usually used as a control in studies to elucidate the effect of KN-93. KN-93 inhibits fibroblast CaMK-II activity and cell growth, whereas KN-92 had no effect on CaMK-II activity or cell growth.

Animal experiment [2]:

Animal models

AC3-I and AC3-C transgenic mice

Dosage form

20 μmol/kg, intraperitoneal

Application

Treatment with KN-93 in WT mice resulted in a dose-dependent improvement in left ventricular function compared to WT mice treated with KN-92. Surviving myocytes from infarcted wild-type mice without treatment or treated with control drug KN-92 exhibited severely disordered Ca2+ homeostasis. In contrast, Ca2+ homeostasis was preserved after myocardial infarction in wild-type mice treated with KN-93.

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]. Tombes R M, Grant S, Westin E H, et al. G1 cell cycle arrest and apoptosis are induced in NIH 3T3 cells by KN-93, an inhibitor of CaMK-II (the multifunctional Ca2+/CaM kinase)[J]. Cell growth & differentiation: the molecular biology journal of the American Association for Cancer Research, 1995, 6(9): 1063.

[2]. Zhang R, Khoo M S C, Wu Y, et al. Calmodulin kinase II inhibition protects against structural heart disease[J]. Nature medicine, 2005, 11(4): 409-417.

Biological Activity

Description KN-92 hydrochloride is a negative control for KN-93.
Targets            
IC50            

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