KN-62 is a cell-permeable, reversible, and selective inhibitor of CaM kinase II (Ki = 900 nM for rat brain CaM kinase II). KN-62 is also a potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM). KN-62 inhibits the growth of K562 cells in a dose-dependent manner. KN-62 could inhibit the Ca2+/CaM kinase II activity in vivo. However, KN-62 only slightly influenced PC secretion from type II cells stimulated by phorbol 12-myristate 13-acetate, terbutaline and ATP that are known to increase surfactant secretion via the protein kinase C and protein kinase A pathways. KN-62 affects the interaction between calmodulin and Ca2+/CaM kinase II following inhibition of this kinase activity by directly binding to the calmodulin binding site of the enzyme but does not affect the calmodulin-independent activity of already autophosphorylated (activated) enzyme.
| Molecular Weight | 721.84 |
| Formula | C38H35N5O6S2 |
| CAS Number | 127191-97-3 |
| Solubility (25°C) | DMSO: ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related CaMK Products |
|---|
| Autocamtide 2
Autocamtide 2 is a highly selective peptide substrate of calcium/calmodulin-dependent protein kinase II (CaMKII). |
| Syntide 2
Syntide 2, a Ca2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected. |
| Autocamtide-2-related inhibitory peptide, myristoylated
Autocamtide-2-related inhibitory peptide, myristoylated is the myristoylated Autocamtide-2-related inhibitory peptide. |
| Calmodulin Dependent Protein Kinase Substrate
Calmodulin Dependent Protein Kinase Substrate is a Ca2+- and calmodulin (CaM)-dependent protein kinase (CaMK) substrate peptide. |
| Calmodulin Dependent Protein Kinase Substrate Analog
Calmodulin Dependent Protein Kinase Substrate Analog is a Ca2+- and calmodulin (CaM)-dependent protein kinase (CaMK) substrate peptide. |
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