KN-93

KN-93 価格

KN-93 化学特性,用途語,生産方法

• 外観

  白色～ほとんど白色, 結晶性粉末～粉末

• 溶解性

  メタノールに溶ける。

• 用途

  阻害剤。

• 説明

  KN-93 is a selective inhibitor of Ca²⁺/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 Ca²⁺-phosphodiesterase. It inhibits histamine-induced aminopyrine uptake in parietal cells (IC₅₀ = 300 nM). 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.

• 化学的特性

  white to off-white powder

• 使用

  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
  
  

• 定義

  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.

• 一般的な説明

  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 G₁ cell cycle arrest and apoptosis in NIH 3T3 cells.

• 生物活性

  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 生産企業

Global(157)Suppliers

KN-93 スペクトルデータ(¹HNMR)

139298-40-1, KN-93 キーワード