Merck
CN
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文件

K1385

Sigma-Aldrich

KN-93

≥98% (HPLC)

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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
经验公式（希尔记法）:
C26H29ClN2O4S · H3PO4
CAS号:
139298-40-1
分子量:
599.03
MDL编号:
MFCD03788201
PubChem化学物质编号:
329817125

生物来源

synthetic (organic)

质量水平

200

检测方案

≥98% (HPLC)

形式

powder

颜色

white

溶解性

DMSO: 1 mg/mL
H2O: soluble

储存温度

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

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应用

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

生化/生理作用

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。

特点和优势

《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。

注意

光敏性

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)

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  • 如果您查询到的批号为 TO09019TO 等，请输入去除前两位字母的批号：09019TO。

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  1. Which document(s) contains shelf-life or expiration date information for a given product?

    If available for a given product, the recommended re-test date or the expiration date can be found on the Certificate of Analysis.

  2. How do I get lot-specific information or a Certificate of Analysis?

    The lot specific COA document can be found by entering the lot number above under the "Documents" section.

  3. How do I find price and availability?

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  4. What is the Department of Transportation shipping information for this product?

    Transportation information can be found in Section 14 of the product's (M)SDS.To access the shipping information for this material, use the link on the product detail page for the product. 

  5. Is Product No. K1385, KN-93, a salt?

    Yes.  It is the phosphate salt.  

  6. What is Product No. K1385, KN-93, soluble in?

    Product K1385 is a water soluble form of KN-93, soluble in water at least at 5 mg/ml. It is also soluble in dimethyl sulfoxide (DMSO) to at least 1 mg/ml.  Solutions and solid should be protected from light.

  7. How to store solutions of Product No. K1385, KN-93?

    Sigma has not performed solution stability studies. However, stock solutions may be stable for 1-3 months, if aliquotted and stored frozen at -20°C.

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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
Differential Responses of Cultured MC3T3-E1 Cells to Dynamic and Static Stimulated Effect of Microgravity in Cell Morphology, Cytoskeleton Structure and Ca2+ Signaling
Luo M, et al.
mBio, 13(2), 137-157 (2016)
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)
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)
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