Biological Activity
Selective, cell-permeable inhibitor of CaM kinase II (IC50 = 0.9 μM). Binds directly to the calmodulin binding site of the enzyme. Potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).
Technical Data
| M. Wt | 721.84 |
| Formula | C38H35N5O6S2 |
| Storage | Desiccate at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 127191-97-3 |
| PubChem ID | 5312126 |
| InChI Key | RJVLFQBBRSMWHX-DHUJRADRSA-N |
| Smiles | O=S(C1=CC=CC2=C1C=CN=C2)(N(C)[C@H](C(N4CCN(C7=CC=CC=C7)CC4)=O)CC3=CC=C(OS(C5=CC=CC6=C5C=CN=C6)(=O)=O)C=C3)=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 | 72.18 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 721.84. 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 | 1.39 mL | 6.93 mL | 13.85 mL |
| 5 mM | 0.28 mL | 1.39 mL | 2.77 mL |
| 10 mM | 0.14 mL | 0.69 mL | 1.39 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.28 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Chessell et al (1998) Effects of antagonists at the human recombinant P2X7 receptor. Br.J.Pharmacol. 124 1314 PMID: 9720806
Hidaka and Yokokura (1996) Molecular and cellular pharmacology of a calcium/calmodulin-dependent protein kinase II (CaM kinase II) inhibitor, KN-62, and proposal of CaM kinase phosphorylation cascades. Adv.Pharmacol. 36 193 PMID: 8783561
Tokumitsu et al (1990) KN-62, 1-[N-O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II. J.Biol.Chem. 265 4315 PMID: 2155222
Keywords: KN-62, supplier, CaM, kinase, II, inhibitors, inhibits, Non-competitive, P2X7, antagonists, Calmodulin-Activated, calmodulin-dependent, Protein, Kinase, Kinases, Ca2+, Binding, modulators, Calcium, Signaling, Signalling, Receptors, Purinergic, purinoceptors, P2X, Receptors, Calcium, Binding, Protein, CaM, Kinase, P2X, Receptors, Tocris Bioscience
