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크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C26H29ClN2O4S · H3PO4
CAS 번호:
Molecular Weight:
599.03
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
제품 이름
KN-93, ≥98% (HPLC)
SMILES string
OP(O)(O)=O.COc1ccc(cc1)S(=O)(=O)N(CCO)c2ccccc2CN(C)C\C=C\c3ccc(Cl)cc3
InChI key
NNKJTPOXLIILMB-IPZCTEOASA-N
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+;
biological source
synthetic (organic)
assay
≥98% (HPLC)
form
powder
color
white
solubility
DMSO: 1 mg/mL
H2O: soluble
storage temp.
2-8°C
Quality Level
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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.
Disclaimer
Photosensitive
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.
저장 등급
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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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
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Li B, et al.
Test, 288(19), 13610-13619 (2013)
Potentiation of Schaffer-Collateral CA1 Synaptic Transmission by eEF2K and p38 MAPK Mediated Mechanisms
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Frontiers in Cellular Neuroscience, 247-247 (2016)
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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
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