KN-92 hydrochloride

Short Summary : Inactive derivative of KN-93,control compound

Category : Membrane Transporter/Ion Channel|P2X purinergic receptor

Purity : 0.9842

CAS Number : 1431698-47-3

Formula : C24H26Cl2N2O3S

Molecular Weight : 493.45

SMILE : ClC1=CC=C(/C=C/CN(C)CC2=CC=CC=C2NS(C3=CC=C(OC)C=C3)(=O)=O)C=C1.Cl

Solubility : >24.7mg/mL in DMSO

Storage : Store at -20°C

Description : 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 M) 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 M), but the inactive analog KN-92 did not (Ki > 100 M). 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.

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