KN-93 (phosphate)

KN-93 (phosphate) is a potent and selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII) (Ki = 370 nM), inhibiting both the alpha- and beta-subunits of CaMKII. It does not have significant effects on cAMP-dependent protein kinase, Ca2+/phospholipid-dependent protein kinase, myosin light chain kinase, or Ca2+ phosphodiesterase activity. It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM). KN-93 can block voltage-gated potassium (Kv) channels when applied extracellularly, independent of its CaMKII action. More recently, 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-1alpha in colon cancer cells.Formal Name: N-[2-[[[(2E)-3-(4-chlorophenyl)-2-propen-1-yl]methylamino]methyl]phenyl]-N-(2-hydroxyethyl)-4-methoxy-benzenesulfonamide, monophosphate. CAS Number: 1188890-41-6. Molecular Formula: C26H29ClN2O4S . H3PO4. Formula Weight: 599.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 30 mg/ml, Ethanol: slightly, PBS (pH 7.2): slightly. lambdamax: 252 nm. SMILES: CN(C/C=C/C1=CC=C(Cl)C=C1)CC2=CC=CC=C2N(S(=O)(C3=CC=C(OC)C=C3)=O)CCO.O=P(OO)=O.[HH]. InChi Code: InChI=1S/C26H29ClN2O4S.HO4P.H2/c1-28(17-5-6-21-9-11-23(27)12-10-21)20-22-7-3-4-8-26(22)29(18-19-30)34(31,32)25-15-13-24(33-2)14-16-25,1-4-5(2)3,/h3-16,30H,17-20H2,1-2H3,1H,1H/b6-5+,,. InChi Key: NKTVVGUNDPPKQD-TXOOBNKBSA-N.