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KN-92

Names

[ CAS No. ]:
176708-42-2

[ Name ]:
KN-92

[Synonym ]:
Benzenesulfonamide, N-[2-[[[(2E)-3-(4-chlorophenyl)-2-propen-1-yl]methylamino]methyl]phenyl]-4-methoxy-
MFCD22628835
N-[2-({[(2E)-3-(4-Chlorophenyl)-2-propen-1-yl](methyl)amino}methyl)phenyl]-4-methoxybenzenesulfonamide

Biological Activity

[Description]:

KN-92 is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM). IC50 value:Target: KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM). KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cell.

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> CaMK
Research Areas >> Others

[References]

[1]. Rokhlin OW, Guseva NV, Taghiyev AF et al. KN-93 inhibits androgen receptor activity and induces cell death irrespective of p53 and Akt status in prostate cancer. Cancer Biol Ther. 2010 Feb;9(3):224-35.

[2]. An P, Zhu JY, Yang Y et al. KN-93, a specific inhibitor of CaMKII inhibits human hepatic stellate cell proliferation in vitro. World J Gastroenterol. 2007 Mar 7;13(9):1445-8.

[3]. Gao L, Blair LA, Marshall J. et al. CaMKII-independent effects of KN93 and its inactive analog KN92: reversible inhibition of L-type calcium channels. Biochem Biophys Res Commun. 2006 Jul 14;345(4):1606-10.

[4]. Rezazadeh S, Claydon TW, Fedida D. et al. 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-

[5]. Anderson ME, Braun AP, Wu Y et al. 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.

[6]. Sumi M, Kiuchi K, Ishikawa T et al. The newly synthesized selective Ca2+/calmodulin dependent protein kinase II inhibitor KN-93 reduces dopamine contents in PC12h cells. Biochem Biophys Res Commun. 1991 Dec 31;181(3):968-75.


[Related Small Molecules]

KN-93 | STO609 | KN-62 | KN-92-hydrochloride | CaMKII-IN-1 | MLCK inhibitor peptide 18 | Autocamtide-2 | A 484954 | Rimacalib | Calmodulin-Dependent Protein Kinase II (290-309) | Metofenazate | NH 125 | Syntide 2 trifluoroacetate salt

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
602.1±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H25ClN2O3S

[ Molecular Weight ]:
456.985

[ Flash Point ]:
317.9±34.3 °C

[ Exact Mass ]:
456.127441

[ LogP ]:
5.97

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.630

[ Storage condition ]:
-20°C


Related Compounds