KN-62

KN-62 화학적 특성, 용도, 생산

• 화학적 성질

  Yellow Solid

• 용도

  It is used as a potent and selective inhibitor of CaMKII. KN-62 has demonstrated potent and selective inhibition of Ca2+/calmodulin-dependent protein kinase II (CaMKII; Ki=0.9 ?M) which causes cells to arrest in the S phase. In HEK-293 cells expressing type III adenylyl cyclase (III-AC), 10 ?M of KN-62 blocked CaMKII phosphorylation of III-AC, and inhibited hormone-stimulated Ca2+ oscillations. Additionally, KN-62 is a potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).

• 일반 설명

  A cell-permeable, reversible, and selective inhibitor of CaM kinase II (K_i = 900 nM for rat brain CaM kinase II) that binds directly to the calmodulin binding site of the enzyme. Also inhibits the growth of K562 cells in a dose-dependent manner.

• 생물학적 활성

  Selective, cell-permeable inhibitor of CaM kinase II (IC 50 = 0.9 μ M). Binds directly to the calmodulin binding site of the enzyme. Potent non-competitive antagonist at the P2X 7 receptor (IC 50 = 15 nM). Also available as part of the Mixed Kinase Inhibitor Tocriset™ .

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