KN-93 C화학적 특성, 용도, 생산
개요
KN-
93 is a selective inhibitor of Ca
2+/calmodulin-
dependent kinase type II (CaMKII), competitively blocking CaM binding to the kinase (K
i = 370 nM). It does not affect the activities of PKA, PKC, MLCK, or Ca
2+-
phosphodiesterase. It inhibits histamine-
induced aminopyrine uptake in parietal cells (IC
50 = 300 nM). More recently, KN-
93 has been used to implicate roles for CaMKII in Ca
2+-
induced Ca
2+ release in cardiac myocytes, constitutive phosphorylation of 5-
lipoxygenase in 3T3 cells, and Ca
2+-
dependent activation of HIF-
1α in colon cancer cells.
화학적 성질
white to off-white powder
용도
KN-93 has been used:
- as an inhibitor to block αCaMKII (Ca2+/calmodulin-dependent protein kinase IIα)
- as CaMKII inhibitor to pre-treat hippocampal slices
- to treat the cells, to alter the cytoskeleton (CSK) structure and function during the experiment
정의
ChEBI: A sulfonamide resulting from the formal condensation of p-methoxybenzenesulfonic acid with the anilino nitrogen of 2-(aminomethyl)-N-(2-hydroxyethyl)aniline in which the hydrogens of the primary amino group have been replace
by methyl and p-chlorocinnamyl groups. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent protein kinase II.
일반 설명
Cell-permeable, reversible, and competitive inhibitor of rat brain Ca
+2/calmodulin-dependent protein kinase II (K
i = 370 nM). KN-93 selectively binds to the Calmodulin (CaM) binding site of the enzyme and prevents the association of CaM with CaM Kinase II. Selectively binds to the CaM binding site of the enzyme and prevents the association of CaM with CaMKII. Has no significant effect on protein kinase A activity. Induces G
1 cell cycle arrest and apoptosis in NIH 3T3 cells.
생물학적 활성
Potent inhibitor of CaM kinase II (IC 50 = 0.37 μ M). Also a direct extracellular open channel blocker of voltage-gated potassium channels (IC 50 = 307 nM for Kv1.5); independent of CaM kinase II inhibition.
KN-93 준비 용품 및 원자재
원자재
준비 용품
