product name KN-62
Description: KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM. KN62 inhibits the invasiveness of cancer cells in vitro and in vivo KN62 causes retrograde amnesia in the rat. KN62 attenuates glutamate release by inhibiting voltage-dependent Ca2+-channels. The effect of KN62 on Ca2+-influx appears to be specific to slowly-or non-inactivating conductances, and therefore presents KN62 as a potentially useful tool.
References: J Biol Chem. 1990 Mar 15;265(8):4315-20; Eur J Neurosci. 1998 Jan;10(1):377-87.
721.84
Formula
C38H35N5O6S2
CAS No.
127191-97-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (138.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403955
| In Vitro |
In vitro activity: KN-62 suppresses the A23187-induced autophosphorylation of Ca2+/CaM kinase in PC12 D cells. KN-62 (10 μM) inhibits carbachol and potassium-stimulated insulin secretion from rat pancreatic islets. KN-62 also inhibits growth of K562 cells and blocks cell cycle progression. Kinase Assay: Total kinase activity of CaMKII, determined in a standard 2 min assay (100 μL), contained 35 mM HEPES, 10 mM MgCl2, 1 mM CaCl2, 10 μg of chicken gizzard myosin 20-kD light chain, 0.1 μM calmodulin, and 10 μM [γ-33]ATP at 30 °C. The kinase reaction is halted by adding 1 mL of 10% trichloroacetic acid. Cell Assay: For cell growth analysis, K562 cells are plated in a 3-cm dish with 5 mL of culture medium containing various concentration of KN-62. After two days in these condition cell numbers are counted. |
|---|---|
| In Vivo | KN-62 inhibits seizure-induced expression of brain-derived neurotrophic factor mRNA in adult rat brain. |
| Animal model | Sprague Dawley Rats |
| Formulation & Dosage | Dissolved in 0.5 mM KN-62/50% DMSO; 2 pmol; intracerebroventricular (ICV) injection |
| References | J Biol Chem. 1990 Mar 15;265(8):4315-20; Eur J Neurosci. 1998 Jan;10(1):377-87. |
Related Posts
product name KN-62
Description: KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM. KN62 inhibits the invasiveness of cancer cells in vitro and in vivo KN62 causes retrograde amnesia in the rat. KN62 attenuates glutamate release by inhibiting voltage-dependent Ca2+-channels. The effect of KN62 on Ca2+-influx appears to be specific to slowly-or non-inactivating conductances, and therefore presents KN62 as a potentially useful tool.
References: J Biol Chem. 1990 Mar 15;265(8):4315-20; Eur J Neurosci. 1998 Jan;10(1):377-87.
721.84
Formula
C38H35N5O6S2
CAS No.
127191-97-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (138.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403955
| In Vitro |
In vitro activity: KN-62 suppresses the A23187-induced autophosphorylation of Ca2+/CaM kinase in PC12 D cells. KN-62 (10 μM) inhibits carbachol and potassium-stimulated insulin secretion from rat pancreatic islets. KN-62 also inhibits growth of K562 cells and blocks cell cycle progression. Kinase Assay: Total kinase activity of CaMKII, determined in a standard 2 min assay (100 μL), contained 35 mM HEPES, 10 mM MgCl2, 1 mM CaCl2, 10 μg of chicken gizzard myosin 20-kD light chain, 0.1 μM calmodulin, and 10 μM [γ-33]ATP at 30 °C. The kinase reaction is halted by adding 1 mL of 10% trichloroacetic acid. Cell Assay: For cell growth analysis, K562 cells are plated in a 3-cm dish with 5 mL of culture medium containing various concentration of KN-62. After two days in these condition cell numbers are counted. |
|---|---|
| In Vivo | KN-62 inhibits seizure-induced expression of brain-derived neurotrophic factor mRNA in adult rat brain. |
| Animal model | Sprague Dawley Rats |
| Formulation & Dosage | Dissolved in 0.5 mM KN-62/50% DMSO; 2 pmol; intracerebroventricular (ICV) injection |
| References | J Biol Chem. 1990 Mar 15;265(8):4315-20; Eur J Neurosci. 1998 Jan;10(1):377-87. |