KN-93 (10 μM) 显著抑制高血糖诱导的 CaMKII/NF-κB 信号通路激活，随后降低 Müller 细胞中血管内皮生长因子 、诱导型一氧化氮合酶 和细胞间黏附分子-1 (ICAM-1) 的表达 。

2019年3月29日 · The molecule KN-93 is the most widely used inhibitor for studying the cellular and in vivo functions of CaMKII. It is widely believed that KN-93 binds directly to CaMKII, thus preventing kinase activation by competing with Ca 2+ /CaM. Herein, we employed surface plasmon resonance, NMR, and isothermal titration calorimetry to characterize this ...

KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM. - Mechanism of Action & Protocol.

2019年3月29日 · Our results revealed that KN-93 binds directly to Ca2+ /CaM and not to CaMKII. This binding would disrupt the ability of Ca 2+ /CaM to interact with CaMKII, effectively inhibiting CaMKII activation. Our findings also indicated that KN-93 can specifically compete with a CaMKIIδ-derived peptide for binding to Ca 2+/CaM.

KN-93 H 3 PO 4 是一种强效的特异性的Ca 2+ /calmodulin-dependent protein kinase II (CaMKII)抑制剂，其Ki为0.37μM，对 APK、PKC、MLCK或Ca 2+ -PDE没有明显的抑制活性。 KN-93抑制PC12h细胞中多巴胺的形成，通过调整TH的反应率，以减少Ca (2+)介导的TH分子磷酸化水平。 KN-93抑制血清诱导的成纤维细胞生长，IC50为8μM，并在延长的G1期阻滞后诱导细胞凋亡。 在PCa 细胞中，KN-93抑制雄激素受体活性和p53单独诱导的细胞死亡。 在患帕金森病的大鼠模 …

KN-93 is a selective inhibitor of Ca (2+)/calmodulin-dependent protein kinase II. It has a role as an EC 2.7.11.17 (Ca (2+)/calmodulin-dependent protein kinase) inhibitor and a geroprotector. It is a sulfonamide, a tertiary amino compound, a primary alcohol, a member of monochlorobenzenes and a monomethoxybenzene.

乙酰胆碱/CHRNA5轴通过CAMKII/GSK3β信号通路增加β-catenin的表达，促进ICC转移和对吉西他滨的耐药，CAMKII抑制剂KN93可能是对抗ICC转移的有效治疗策略。 https://www.nature.com/articles/s41392-024-01761-z#Sec9 研究背景 01 肝内胆管癌 (ICC)约占原发性肝脏恶性肿瘤的5-10%，其发病率在全球范围内呈上升趋势。

2019年7月28日 · KN-93 hydrochloride是可渗透细胞，可逆和竞争性的抑制剂钙调蛋白依赖性激酶II型 (CaMKII) 抑制剂，Ki 为370 nM。 - 高纯度，全球文献引用。 — Master of Bioactive Molecules

Treatment of MRL/lpr Foxp3-GFP mice with KN-93 results in a significant induction of Treg cells in the spleen, peripheral lymph nodes and peripheral blood and this is accompanied by decreased skin and kidney damage. Notably, KN-93 clearly diminishes the accumulation of inflammatory cells along with reciprocally increased Treg cells in target organ.