A CaMKK inhibitor
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STO-609 is a calcium/calmodulin-dependent protein kinase kinase (CaMKK) inhibitor (IC50s = 120 and 40 ng/ml for CaMKKα and CaMKKβ, respectively).1 It is selective for CaMKKs over CaMKI, CaMKII, CaMKIV, MLCK, PKC, PKA, and p42 MAPK (IC50s = ≥10,000 ng/ml for all). STO-609 inhibits phosphorylation of CaMKI and AMP-activated protein kinase (AMPK) in chicken sperm in the presence of extracellular calcium, as well as reduces chicken sperm motility, in a concentration-dependent manner.2 It decreases hypothalamic neuropeptide Y (Npy) and agouti-related protein (Agrp) expression and cumulative food intake in mice when administered intracerebroventricularly as a 20 μM solution at a continuous rate of 0.5 μL/hour .3 STO-609 (3 μg/animal, i.c.v.) increases cortical, striatal, and total infarct volume in a mouse model of focal transient cerebral ischemia induced by middle cerebral artery occlusion (MCAO).4
1.Tokumitsu, H., Inuzuka, H., Ishikawa, Y., et al.STO-609, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase kinaseJ. Biol. Chem.278(13)10908-10913(2013) 2.Nguyen, T.M.D., Combarnous, Y., Praud, C., et al.Ca2+/calmodulin-dependent protein kinase kinases (CaMKKs) effects on AMP-activated protein kinase (AMPK) regulation of chicken sperm functionsPLoS One11(1)e0147559(2016) 3.Anderson, K.A., Ribar, T.J., Lin, F., et al.Hypothalamic CaMKK2 contributes to the regulation of energy balanceCell Metab.7(5)377-388(2008) 4.McCullough, L.D., Tarabishy, S., Liu, L., et al.Inhibition of calcium/calmodulin-dependent protein kinase kinase β and calcium/calmodulin-dependent protein kinase IV is detrimental in cerebral ischemiaStroke44(9)2559-2566(2013)
Dorsomorphin (Compound C) 2HCl
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