 | |
| Names | |
|---|---|
| Preferred IUPAC name 4-[(2S)-2-(N-Methylisoquinoline-5-sulfonamido)-3-oxo-3-(4-phenylpiperazin-1-yl)propyl]phenyl isoquinoline-5-sulfonate | |
| Identifiers | |
3D model (JSmol) | |
| ChemSpider | |
| MeSH | C063302 |
| UNII | |
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| Properties | |
| C38H35N5O6S2 | |
| Molar mass | 721.84 g/mol |
| Boiling point | 964.7±75.0 °C at 760 mmHg |
| Hazards | |
| Flash point | 537.3±37.1 °C |
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). | |
KN-62 is a derivative of isoquinolinesulfonamide, it is a selective, specific and cell permeable inhibitor ofCa2+/calmodulin-dependent kinase type II (CaMK II) withIC50 of 900nM,[1] charactered byhydrophobicity. KN-62 also potently inhibits thepurinergic receptorP2X7.[2]
KN-62 blocks the combination of CaM and CaMK II by binding directly to thecalmodulin binding site of theenzyme, disenables CaMK II'sautophosphorylation, consequently leading inactivation.Kinetic analysis exhibits that this inhibitory effect of KN-62 is competitive with respect to calmodulin.[3] Since KN-62 binds to the calmodulin binding site of CaMK II, KN-62 doesn't inhibit activity of autophosphorylated CaMK II.
Besides, KN-62 also acts as a potent non-competitiveantagonist at thepurinergic receptorP2RX7 withIC50 of 15nM.
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