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KN-93 is a methoxybenzenesulfonamide that is an effective inhibitor of CaMKII (Ca2+/calmodulin-dependent protein kinase II) phosphorylating activity, and the autophosphorylation of the α- and β-subunits of CaMKII. In PC-12h cells, KN-93 has been shown to decrease phosphorylation of KCl and acetylcholine. Data suggests that KN-93 modulates the reaction rate of TH by reducing the Ca2+ mediated phosphorylation levels of TH and inhibiting dopamine formation. In rat pancreatic beta cell studies, KN-93 was shown to block insulin release, and in prostrate cancer research, KN-93 inhibited androgen receptor function and enhanced cell death independent of p53 and Akt. Research indicates that KN-93 induces G1 cell cycle arrest in both HeLa (sc-2200) and NIH 3T3 fibroblast cells (sc-2210), and causes apoptosis in NIH 3T3 cells.
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See how others have used KN-93. Click on the entry to view the PubMed entry .
PMID: # 27012864
Gu, Y. et al. 2016. Aberrant activation of CaMKIIγ accelerates chronic myeloid leukemia blast crisis. Leukemia.
PMID: # 24863146
Pagani, JH. et al. 2015. Role of the vasopressin 1b receptor in rodent aggressive behavior and synaptic plasticity in hippocampal area CA2. Mol. Psychiatry. 20: 490-9.
PMID: # 25042347
Diniz, LP. et al. 2014. Astrocyte transforming growth factor beta 1 promotes inhibitory synapse formation via CaM kinase II signaling. Glia. 62: 1917-31.
PMID: # 24993295
Chae, YJ. et al. 2014. Block of Kv4.3 potassium channel by trifluoperazine independent of CaMKII. Neurosci. Lett.. 578: 159-64.
PMID: # 23345405
Seward, ME. et al. 2013. Amyloid-β signals through tau to drive ectopic neuronal cell cycle re-entry in Alzheimer's disease. J. Cell. Sci.. 126: 1278-86.
PMID: # 18978352
Flamand, N. et al. 2009. Phosphorylation of serine 271 on 5-lipoxygenase and its role in nuclear export. J. Biol. Chem.. 284: 306-313.
PMID: # 12933808
Gardoni, F. et al. 2003. CaMKII-dependent phosphorylation regulates SAP97/NR2A interaction. J. Biol. Chem.. 278: 44745-44752.
PMID: # 11782425
Arnould, T. et al. 2002. CREB activation induced by mitochondrial dysfunction is a new signaling pathway that impairs cell proliferation EMBO J. 21(1): 53-63.
PMID: # 11397804
Wheeler, DG. et al. 2001. Depolarization strongly induces human cytomegalovirus major immediate-early promoter/enhancer activity in neurons. J. Biol. Chem.. 276: 31978-31985.
PMID: # 9388275
Ramirez, MT. et al. 1997. The nuclear deltaB isoform of Ca2+/calmodulin-dependent protein kinase II regulates atrial natriuretic factor gene expression in ventricular myocytes. J. Biol. Chem.. 272: 31203-31208.
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