KN-93 Phosphate Chemical Properties

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

KN-93 Phosphate Usage And Synthesis

Description

KN-93 (phosphate) is a potent and selective inhibitor of Ca²⁺/calmodulin-dependent kinase II (CaMKII) (K_i = 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 (K_v) 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

KN 93 Phosphate is a potent and selective inhibitor of Ca2+/calmodulin-dependent protein kinase II.

IC 50

CaMK IIα

storage

-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

KN-93 Phosphate(1188890-41-6)Related Product Information

• KN-62
• Aprepitant
• 1,9-Pyrazoloanthrone
• PD 0332991 HCl
• Veliparib
• CHIR-99021