Molecular Formula | C19H10N2O3 |
Molar Mass | 314.29 |
Density | 1.54±0.1 g/cm3(Predicted) |
Melting Point | >300°C |
Boling Point | 716.9±62.0 °C(Predicted) |
Solubility | DMSO: 15mg/mL at≥60°C |
Appearance | solid |
pKa | 2.65±0.20(Predicted) |
Storage Condition | Sealed in dry,2-8°C |
In vitro study | STO-609 inhibited the activity of recombinant CaM-KKα and CaM-KKβ with Ki values of 80 ng/ml and 15 ng/ml, respectively, and STO-609 also inhibited their autophosphorylation activity. STO-609 is highly selective for CaM-KK and has no significant effect on its downstream CaM Kinase (CaM-KI and -IV). In transfected Hela cells, STO-609 inhibited Ca in a dose-dependent manner. |
In vivo study | Administration to adult mice in vivo, STO-609 will cause the increase of osteoblasts, osteoclast reduction, the ovariectomy induced osteoporosis has a protective effect. Intracerebroventricular injection of STO-609 did not affect the negative regulatory response to neurohypoglycemia or the activation of AMPK by hypoglycemia. |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.182 ml | 15.909 ml | 31.818 ml |
5 mM | 0.636 ml | 3.182 ml | 6.364 ml |
10 mM | 0.318 ml | 1.591 ml | 3.182 ml |
5 mM | 0.064 ml | 0.318 ml | 0.636 ml |
biological activity | STO-609 is a specific CaM-KK inhibitor that inhibits the activity of CaM-KKα and CaM-KKβ, ki values were 80 ng/ml and 15 ng/ml, respectively, and inhibited its autophosphorylation activity. STO-609 can inhibit AMPK activity and inhibit autophagy. |
Target | TargetValue AMPK () CaM-KKβ (Cell-free assay) 47 nM(Ki) caM-KKα (Cell-free assay) 0.25 μm (Ki) |
Target | Value |
AMPK () | |
CaM-KKβ (Cell-free assay) | 47 nM(Ki) |
CaM-KKα (Cell-free assay) | 0.25 μM(Ki) |
in vitro study | STO-609 inhibits the activity of recombinant CaM-KKα and CaM-KKβ, ki values were 80 ng/ml and 15 ng/ml, respectively, and STO-609 also inhibited their autophosphorylation activity. STO-609 is highly selective for CaM-KK and has no significant effect on its downstream CaM Kinase (CaM-KI and -IV). In transfected Hela cells, STO-609 inhibited Ca in a dose-dependent manner. |
in vivo study | in vivo administration to adult mice, STO-609 can cause the increase of osteoblasts and the decrease of osteoclasts, it has a protective effect on osteoporosis caused by ovariectomy. Intracerebroventricular injection of STO-609 did not affect the negative regulatory response to neurohypoglycemia or the activation of AMPK by hypoglycemia. |
Use | a specific CaM-KK inhibitor that inhibits both CaM-KKα and CaM-KKβ, ki values were 80ng/ml and 15ng/ml, respectively, and inhibited its autophosphorylation activity. STO-609 is a specific inhibitor of the Ca(2 )/calmodulin-dependent protein kinase kinase. STO-609 inhibits the activities of recombinant CaM-KK alpha and CaM-KK beta isoforms, with K( I) values of 80 and 15 ng/ml, respectively and also inhibits their autophosphorylation activities. STO-609 is highly selective for CaM-KK without any significant effect on the downstream CaM kinases (CaM-KI and -IV), and the IC(50) value of the compound against CaM-KII is approximately 10 microg/ml. STO-609 is a selective and cell-permeable inhibitor of CaM-KK and that it may be a useful tool for evaluating the physiological significance of the CaM-KK-mediated pathway in vivo as well as in vitro. |