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KN-62

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Chemical Structure| 127191-97-3 同义名 : -
CAS号 : 127191-97-3
货号 : A455366
分子式 : C38H35N5O6S2
纯度 : 98%
分子量 : 721.844
MDL号 : MFCD00083180
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(145.46 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • CaMKII

    CaMKII, Ki:0.9 μM
描述 KN-62 exhibits strong antagonism against ATP-induced Ba2+ influx in fura-2-loaded human lymphocytes, with an IC50 of 12.7 nM and complete inhibition of the flux at a concentration of 500 nM[1]. KN-62 does not hinder the activity of autophosphorylated Ca2+/CaM kinase II. It dose-dependently inhibits the Ca2+/calmodulin-dependent autophosphorylation of both alpha (50 kDa) and beta (60 kDa) subunits of Ca2+/CaM kinase II in the presence or absence of exogenous substrate[2]. KN-62 in human leukemic B lymphocytes diminishes the rate of permeability increase to larger permeant cations, such as ethidium, induced by Bz-ATP, with an IC50 of 13.1 nM[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HEK293 cells Function assay Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium influx, IC50=50.12 nM 19191585
human lymphocytes Function assay Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced Ba2+ influx, IC50=12.59 nM 19191585
THP1 cells Function assay Inhibition of Bz-ATP-induced IL1-beta release in LPS/IFN-gamma-differentiated human THP1 cells by ELISA, IC50=0.081 μM 19110420
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.39mL

0.28mL

0.14mL

6.93mL

1.39mL

0.69mL

13.85mL

2.77mL

1.39mL
参考文献

[1]Gargett CE, et al. The isoquinoline derivative KN-62 a potent antagonist of the P2Z-receptor of human lymphocytes. Br J Pharmacol. 1997 Apr;120(8):1483-90.

[2]H Hidaka, et al. Pharmacology of protein kinase inhibitors. Annu Rev Pharmacol Toxicol. 1992;32:377-97.

[3]Miso Park, et al. Involvement of the P2X7 receptor in the migration and metastasis of tamoxifen-resistant breast cancer: effects on small extracellular vesicles production. Sci Rep. 2019 Aug 12;9(1):11587.

[4]Ravi RG, et al. Potent P2X7 Receptor Antagonists: Tyrosyl Derivatives Synthesized Using a Sequential Parallel Synthetic Approach. Drug Dev Res. 2001 Oct;54(2):75-87.

[5]Manosso LM, et al. Antidepressant-like effect of zinc is dependent on signaling pathways implicated in BDNF modulation. Prog Neuropsychopharmacol Biol Psychiatry. 2015 Jun 3;59:59-67.