STO-609

一种CaMKK抑制剂（对CaMKKα和CaMKKβ的IC50分别为120ng/ml和40ng/ml）；对CaMKK的选择性高于CaMKI、CaMKII、CaMKIV、MLCK、PKC、PKA和p42 MAPK（对这些酶的IC50均≥10,000ng/ml）；在体外钙存在的情况下，抑制鸡精子中CaMKI和AMPK的磷酸化，并降低鸡精子的运动能力；在小鼠中，通过脑室内注射（0.5µL/h，20µM），减少Npy和Agrp的表达以及累积食物摄入量；在小鼠大脑中动脉闭塞（MCAO）诱导的局灶性短暂性脑缺血模型中，以3µg/动物的剂量通过脑室内注射，增加皮层、纹状体和总梗死体积。A CaMKK inhibitor (IC50s = 120 and 40 ng/ml for CaMKKα and CaMKKβ, respectively); selective for CaMKKs over CaMKI, CaMKII, CaMKIV, MLCK, PKC, PKA, and p42 MAPK (IC50s = ≥ 10,000 ng/ml for all); inhibits phosphorylation of CaMKI and AMPK in chicken sperm in the presence of extracellular calcium, as well as reduces chicken sperm motility; decreases Npy and Agrp expression and cumulative food intake in mice at 20 μM 0.5 μL/hour, i.c.v.; increases cortical, striatal, and total infarct volume in a mouse model of MCAO-induced focal transient cerebral ischemia at 3 μg/animal, i.c.v.分子式C19H10N2O3分子量314.3O=C(C(C=CC(C1=NC2=C(N13)C=CC=C2)=C45)=C4C=CC=C5C3=O)O.O=C(C6=CC=C7)N8C9=C(C=CC=C9)N=C8C%10=C6C7=CC(C(O)=O)=C%10