|N-(2-(((3-(4-氯苯基)烯丙基)(甲基)氨基)甲基)苯基)-N-(2-羟乙基)-4-甲氧基苯磺酰胺|CsnPharm

CAS No.: 139298-40-1

KN-93 Catalog No. CSN11255

Synonyms: KN-93

KN-93 is a potent Ca2+/calmodulin-dependent protein kinase II (CaMKII) selective inhibitor with Ki of 370 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CaM/CaMKII

Ki:370nM
描述KN-93 is a CaMKII (Calcium/calmodulin-dependent protein kinase II) blocker. It elicited potent inhibitory effects on CaMKII phosphorylating activity with an inhibition constant of 0.37μM but had no significant effects on the catalytic activity of CAMP-dependent protein kinase, Ca²⁺/phospholipid dependent protein kinase, myosin light chain kinase and Ca²⁺-phosphodiesterase. KN-93 also inhibited the autophosphorylation of both the α- and β-subunits of CaMKII. KN-93 inhibited dopamine formation by modulating the reaction rate of TH to reduce the Ca²⁺-mediated phosphorylation levels of the tyrosine hydroxylase molecule in PC12h cells^[4]. KN-93 also works as a direct extracellular blocker of voltage-gated potassium channels with IC50 value of 307±12nM for block of the Kv1.5. KN-93 acted through promotion and stabilization of C-type inactivation. KN-93 was ineffective as a blocker when applied intracellularly, suggesting that CaMK II-independent effects of KN-93 on Kv channels can be circumvented by intracellular application of KN-93^[5]. KN-93 inhibits I_Kr in mammalian cardiomyocytes^[6].
作用机制KN-93 inhibits CaMKII in a competitive fashion against calmodulin.^[4]
动物研究
剂量
Rat: 1 mg/kg^[4] (i.p.) Woodchucks: 125 mg/kg/h^[5] (i.v.) Mice: 1.5 mg/kg (i.p.), 5 mg/kg^[6] (i.p.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Rat: 1 mg/kg^[4] (i.p.) Woodchucks: 125 mg/kg/h^[5] (i.v.) Mice: 1.5 mg/kg (i.p.), 5 mg/kg^[6] (i.p.)
给药途径	i.p., i.v.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9959 mL
- 9.9793 mL
- 19.9586 mL
- 5 mM
- 0.3992 mL
- 1.9959 mL
- 3.9917 mL
- 10 mM
- 0.1996 mL
- 0.9979 mL
- 1.9959 mL

技术信息

CAS号

139298-40-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H29ClN2O4S

运输

蓝冰

分子量

501.04

别名

KN-93

溶解度

DMSO	100.0 mg/mL (199.6 mM)
Water	Insoluble
Ethanol	20.0 mg/mL (39.9 mM)

动物实验配方

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KN-93 Catalog No. CSN11255

靶点选择性

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