| Identification | Back Directory | [Name]
KN-93 Phosphate | [CAS]
1188890-41-6 | [Synonyms]
CS-1902
KN 93; KN93
KN-93PHOSPHATE
KN-93 phospate
(E)-KN-93 (phosphate)
KN-93 phosphate, >=98%
KN 93 Phosphate (E-form)
KN-93 Phosphate USP/EP/BP
(E)-N-(2-(((3-(4-Chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide phosphate
N-[2-[[[3-(4-Chlorophenyl)-2-propenyl]methylamino]methyl]phenyl]-N-(2-hydroxyethyl)-4-methoxybenzenesulphonamide phosphate
N-[2-({[(2E)-3-(4-Chlorophenyl)-2-propen-1-yl](methyl)amino}methyl)phenyl]-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide phosphate (1:1)
Benzenesulfonamide, N-[2-[[[(2E)-3-(4-chlorophenyl)-2-propen-1-yl]methylamino]methyl]phenyl]-N-(2-hydroxyethyl)-4-methoxy-, phosphate (1:1)
N-[2-[[[3-(4-Chlorophenyl)-2-propenyl]methylamino]methyl]phenyl]-N-(2-hydroxyethyl)-4-
methoxybenzenesulphonamide phosphate KN-93 Phosphate | [Molecular Formula]
C26 H29 Cl N2 O4 S . H3 O4 P | [MDL Number]
MFCD03788201 | [MOL File]
1188890-41-6.mol | [Molecular Weight]
599.033 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,Room Temperature | [solubility ]
DMF:25.0(Max Conc. mg/mL);41.73(Max Conc. mM)
DMSO:76.67(Max Conc. mg/mL);127.98(Max Conc. mM)
Water:49.33(Max Conc. mg/mL);82.35(Max Conc. mM) | [form ]
White to off-white solid. | [color ]
White to off-white | [Water Solubility ]
Soluble in water (10mM) | [CAS DataBase Reference]
1188890-41-6 |
| Hazard Information | Back Directory | [Description]
KN-93 (phosphate) is a potent and selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII) (Ki = 370 nM), inhibiting both the α- and β-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-1α in colon cancer cells. | [Uses]
Selective inhibitor of rat brain Ca2+/calmodulin-dependent protein kinase II. Inhibits glucose-induced and forskolin-stimulated insulin release from isolated pancreatic islets of Langerhans. Has no significant effect on protein kinase A (PKA) activity. Induces G1 cell cycle arrest and apoptosis in NIH 3T3 cells. | [IC 50]
CaMK IIα | [storage]
Store at -20°C | [References]
[1] MARIKO SUMI . The newly synthesized selective Ca2+calmodulin dependent protein kinase II inhibitor KN-93 reduces dopamine contents in PC12h cells[J]. Biochemical and biophysical research communications, 1991, 181 3: Pages 968-975. DOI: 10.1016/0006-291x(91)92031-e
[2] N. MAMIYA. Inhibition of Acid Secretion in Gastric Parietal Cells by the Ca2+/ Calmodulin-Dependent Protein Kinase II Inhibitor KN-93.[J]. Japanese journal of pharmacology, 1994, 10 2 1: 90. DOI: 10.1016/s0021-5198(19)50001-4
[3] SAMAN REZAZADEH D F Thomas W Claydon. 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]. Journal of Pharmacology and Experimental Therapeutics, 2006, 317 1: 292-299. DOI: 10.1124/jpet.105.097618
[4] EMILY A OESTREICH. Epac and phospholipase Cepsilon regulate Ca2+ release in the heart by activation of protein kinase Cepsilon and calcium-calmodulin kinase II.[J]. The Journal of Biological Chemistry, 2009, 284 3: 1514-1522. DOI: 10.1074/jbc.m806994200
[5] NICOLAS FLAMAND. Phosphorylation of serine 271 on 5-lipoxygenase and its role in nuclear export.[J]. Mobilities, 2009, 12 1: 306-313. DOI: 10.1074/jbc.m805593200
[6] C RIGANTI. Artemisinin induces doxorubicin resistance in human colon cancer cells via calcium-dependent activation of HIF-1α and P-glycoprotein overexpression[J]. British Journal of Pharmacology, 2009, 156 7: 1054-1066. DOI: 10.1111/j.1476-5381.2009.00117.x |
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