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Merck
CN

K1385

KN-93

synthetic (organic), ≥98% (HPLC),  Ca2+/calmodulin-dependent protein kinase II inhibitor, powder

别名:

N-[2-[N-(4-氯肉桂)-N-甲基氨基甲基]苯基]-N-(2-羟乙基)-4-甲氧基苯磺酰胺 磷酸盐, N-[2-[[[3-(4′-氯苯基)-2-丙烯基]甲基氨基]甲基]苯基]-N-(2-羟基乙基)-4′-甲氧基苯磺酰胺 磷酸盐

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关于此项目

经验公式(希尔记法):
C26H29ClN2O4S · H3PO4
化学文摘社编号:
分子量:
599.03
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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产品名称

KN-93, ≥98% (HPLC)

biological source

synthetic (organic)

Quality Level

assay

≥98% (HPLC)

form

powder

color

white

solubility

DMSO: 1 mg/mL, H2O: soluble

storage temp.

2-8°C

SMILES string

OP(O)(O)=O.COc1ccc(cc1)S(=O)(=O)N(CCO)c2ccccc2CN(C)C\C=C\c3ccc(Cl)cc3

InChI

1S/C26H29ClN2O4S.H3O4P/c1-28(17-5-6-21-9-11-23(27)12-10-21)20-22-7-3-4-8-26(22)29(18-19-30)34(31,32)25-15-13-24(33-2)14-16-25;1-5(2,3)4/h3-16,30H,17-20H2,1-2H3;(H3,1,2,3,4)/b6-5+;

InChI key

NNKJTPOXLIILMB-IPZCTEOASA-N

Application

KN-93已用于以下情形:
  • 作为抑制剂,阻挡αCaMKII (Ca2+/钙调蛋白依赖性蛋白激酶IIα)
  • 作为CaMKII抑制剂,用于预处理海马脑片
  • 在实验中处理细胞,修改细胞骨架(CSK)结构和功能

Biochem/physiol Actions

KN-93是一种选择性Ca2+/钙调蛋白依赖性蛋白激酶II抑制剂。
KN-93是一种选择性Ca2+/钙调蛋白依赖性蛋白激酶II抑制剂,它参与调节平滑肌收缩。。KN-93预处理可抑制CaM激酶II活化(IC50 ~1 μM)。KN-93可抑制组胺诱导的强直力维持,而在整个时间进程中早期力量发展和MLC20磷酸化反应未受影响。KN-93抑制了KCl刺激的力量发展和维持。KN-93也能抑制KCl诱导的MLC20磷酸化快速增加,而稳态MLC20磷酸化反应不受影响。相反,佛波醇12,13-二丁酸酯(PDBu)不能激活CaM激酶II,而PDBu刺激的力量发展不受KN-93影响。因此,KN-93可能靶向生理刺激诱导的力量维持所必需的阶段,这表明CaM激酶II可在调节动脉平滑肌的强直收缩反应中发挥作用。蛋白激酶C的药理活性不经过KN-93敏感阶段。

Features and Benefits

《受体分类和信号转导》手册的 Ca/CaMKs 页面有该化合物的介绍。想要浏览手册的其他页面, 请单击此处

Disclaimer

光敏性

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


历史批次信息供参考:

分析证书(COA)

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Thomas Hennig et al.
PLoS pathogens, 14(3), e1006954-e1006954 (2018-03-27)
Lytic herpes simplex virus 1 (HSV-1) infection triggers disruption of transcription termination (DoTT) of most cellular genes, resulting in extensive intergenic transcription. Similarly, cellular stress responses lead to gene-specific transcription downstream of genes (DoG). In this study, we performed a
Potentiation of Schaffer-Collateral CA1 Synaptic Transmission by eEF2K and p38 MAPK Mediated Mechanisms
Weng W, et al.
Frontiers in Cellular Neuroscience, 247-247 (2016)
S Tessier et al.
Circulation research, 85(9), 810-819 (1999-10-26)
Ca(2+)/calmodulin-dependent protein kinases II (CaMKII) have important functions in regulating cardiac excitability and contractility. In the present study, we examined whether CaMKII regulated the transient outward K(+) current (I(to)) in whole-cell patch-clamped human atrial myocytes. We found that a specific
Kristen H Jardine et al.
Scientific reports, 10(1), 9209-9209 (2020-06-10)
Reactivated long-term memories can become labile and sensitive to modification. Memories in this destabilized state can be weakened or strengthened, but there is limited research characterizing the mechanisms underlying retrieval-induced qualitative updates (i.e., information integration). We have previously implicated cholinergic
Wingless-type mammary tumor virus integration site family, member 5A (Wnt5a) regulates human immunodeficiency virus type 1 (HIV-1) envelope glycoprotein 120 (gp120)-induced expression of pro-inflammatory cytokines via the Ca2+/calmodulin-dependent protein kinase II (CaMKII) and c-Jun N-terminal kinase (JNK) signaling pathways
Li B, et al.
Test, 288(19), 13610-13619 (2013)

全球贸易项目编号

货号GTIN
K1385-.1MG04061833867952
K1385-.5MG04061833867969

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