K1385
KN-93
synthetic (organic), ≥98% (HPLC), Ca2+/calmodulin-dependent protein kinase II inhibitor, powder
Synonym(s):
N-[2-[N-(4-Chlorocinnamyl)-N-methylaminomethyl]phenyl]-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide phosphate salt, N-[2-[[[3-(4′-Chlorophenyl)-2-propenyl]methylamino]methyl]phenyl]-N-(2-hydroxyethyl)-4′-methoxybenzenesulfonamide phosphate salt
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About This Item
Empirical Formula (Hill Notation):
C26H29ClN2O4S · H3PO4
CAS Number:
Molecular Weight:
599.03
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Product Name
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 has been used:
- as an inhibitor to block αCaMKII (Ca2+/calmodulin-dependent protein kinase IIα)
- as CaMKII inhibitor to pre-treat hippocampal slices
- to treat the cells, to alter the cytoskeleton (CSK) structure and function during the experiment
Biochem/physiol Actions
KN-93 is a selective Ca2+/calmodulin-dependent protein kinase II inhibitor, which has been implicated in the regulation of smooth muscle contractility. CaM kinase II activation was inhibited by KN-93 pretreatment (IC50 ~1 μM). KN-93 inhibited histamine-induced tonic force maintenance, whereas early force development and MLC20 phosphorylation responses during the entire time course were unaffected. Both force development and maintenance in response to KCl were inhibited by KN-93. Rapid increases in KCl-induced MLC20 phosphorylation were also inhibited by KN-93, whereas steady-state MLC20 phosphorylation responses were unaffected. In contrast, phorbol 12,13-dibutyrate (PDBu) did not activate CaM kinase II and PDBu-stimulated force development was unaffected by KN-93. Thus KN-93 appears to target a step(s) essential for force maintenance in response to physiological stimuli, suggesting a role for CaM kinase II in regulating tonic contractile responses in arterial smooth muscle. Pharmacological activation of protein kinase C bypasses the KN-93 sensitive step.
KN-93 is a selective Ca2+/calmodulin-dependent protein kinase II inhibitor.
Features and Benefits
This compound is featured on the Ca/CaMKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Disclaimer
Photosensitive
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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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
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
Jing Xu et al.
Advanced science (Weinheim, Baden-Wurttemberg, Germany), 6(8), 1801233-1801233 (2019-04-25)
Fullerene C60 nanocrystals (nano-C60) possess various attractive bioactivities, including autophagy induction and calcium/calmodulin-dependent protein kinase IIα (CaMKIIα) activation. CaMKIIα is a multifunctional protein kinase involved in many cellular processes including tumor progression; however, the biological effects of CaMKIIα activity modulated
Global Trade Item Number
| SKU | GTIN |
|---|---|
| K1385-.1MG | 04061833867952 |
| K1385-.5MG | 04061833867969 |