KN92(KN-92)|cas 1135280-28-2|DC Chemicals

Cas No.:	1135280-28-2
Chemical Name:	KN-92 phosphate
Synonyms:	KN 92; KN92
SMILES:	O=S(C1=CC=C(OC)C=C1)(NC2=CC=CC=C2CN(C/C=C/C3=CC=C(Cl)C=C3)C)=O.O=P(O)(O)O
Formula:	C₂₄H₂₈ClN₂O₇PS
M.Wt:	554.979
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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).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.

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-gated potassium channels. J Pharmacol Exp Ther. 2006 Apr;317(1):292-9. [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. [7]. Park SW, et al. CRABP1 protects the heart from isoproterenol-induced acute and chronic remodeling. J Endocrinol. 2018 Mar;236(3):151-165.

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KN92 phosphate