Biological Activity
Potent, cell permeable inhibitor of CaM kinase II (IC50 = 0.37 μM). Also a direct extracellular open channel blocker of voltage-gated potassium channels (IC50 = 307 nM for KV1.5) and abolishes IKr in ventricular myocytes (IC50 = 102.6 nM) independently of CaM kinase II inhibition. Water soluble form also available.
Technical Data
| M. Wt | 501.04 |
| Formula | C26H29ClN2O4S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 139298-40-1 |
| PubChem ID | 5312122 |
| InChI Key | LLLQTDSSHZREGW-AATRIKPKSA-N |
| Smiles | O=S(N(CCO)C1=C(CN(C)C/C=C/C3=CC=C(Cl)C=C3)C=CC=C1)(C2=CC=C(OC)C=C2)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.1 | 100mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 501.04. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2 mL | 9.98 mL | 19.96 mL |
| 5 mM | 0.4 mL | 2 mL | 3.99 mL |
| 10 mM | 0.2 mL | 1 mL | 2 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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References
References are publications that support the products' biological activity.
Patel et al (1999) Calcium/calmodulin-dependent phosphorylation and activation of human Cdc25-C at the G2/M phase transition in HeLa cells. J.Biol.Chem. 274 7958 PMID: 10075693
Rezazadeh et al (2006) KN-93 (2-[N-(2-Hydroxyethyl)]-N-(4-methoxybenzenesulfonyl)]-amino-N-(4-chlorocinnamyl)-N-methylbenzylamine), a calcium/calmodulin-dependent protein kinase II inhibitor, is a direct extracellular blocker of voltage-gated J.Pharmacol.Exp.Ther. 317 292 PMID: 16368898
Sumi et al (1991) The newly synthesized selective Ca2+/calmodulin dependent protein kinase II inhibitor KN-93 reduces dopamine content in PC12h cells. Biochem.Biophys.Res.Comm. 181 968 PMID: 1662507
Hegyi et al (2015) KN-93 inhibits IKr in mammalian cardiomyocytes. J.Mol.Cell.Cardiol. 89 173 PMID: 26463508
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