It is used as a potent and selective inhibitor of CaMKII. KN-62 has demonstrated potent and selective inhibition of Ca2+/calmodulin-dependent protein kinase II (CaMKII; Ki=0.9 ?M) which causes cells to arrest in the S phase. In HEK-293 cells expressing type III adenylyl cyclase (III-AC), 10 ?M of KN-62 blocked CaMKII phosphorylation of III-AC, and inhibited hormone-stimulated Ca2+ oscillations. Additionally, KN-62 is a potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).
This Thermo Scientific Chemicals brand product was originally part of the Alfa Aesar product portfolio. Some documentation and label information may refer to the legacy brand. The original Alfa Aesar product / item code or SKU reference has not changed as a part of the brand transition to Thermo Scientific Chemicals.
Applications
It is used as a potent and selective inhibitor of CaMKII. KN-62 has demonstrated potent and selective inhibition of Ca2+/calmodulin-dependent protein kinase II (CaMKII; Ki=0.9 μM) which causes cells to arrest in the S phase. In HEK-293 cells expressing type III adenylyl cyclase (III-AC), 10 μM of KN-62 blocked CaMKII phosphorylation of III-AC, and inhibited hormone-stimulated Ca2+ oscillations. Additionally, KN-62 is a potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).
Solubility
Soluble in 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin (0.93 mg/ml), methanol (10 mg/ml), DMSO (12 mg/ml), chloroform (20 mg/ml), ethanol (∼1 mg/ml), 1:2 DMF:PBS (pH 7.2) (∼0.3 mg/ml), and DMF & DMSO (∼30 mg/ml).
Notes
Store in cool place. Keep container tightly closed in a dry and well-ventilated place. Recommended storage temperature: -20°C. Keep away from strong oxidizing agents.
RUO – Research Use Only
General References:
- Okazaki K et al. KN-62, a specific Ca++/calmodulin-dependent protein kinase inhibitor, reversibly depresses the rate of beating of cultured fetal mouse cardiac myocytes. J Pharmacol Exp Ther. 1994, 270, (3), 1319-24.
- Tokumitsu et al. 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.. 1990, 265, (8), 4315-20.