52029-86-4

一种特异性的CaM-KK的抑制剂，抑制CaM-KKα和CaM-KKβ，Ki值分别为80ng/ml和15ng/ml，并抑制其自身磷酸化活性。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.

STO-609 是特异性的CaM-KK的抑制剂，抑制CaM-KKα和CaM-KKβ的活性，Ki值分别为80 ng/ml和15 ng/ml，并抑制其自身磷酸化活性。STO-609 可抑制 AMPKK 活性并抑制自噬。

Target	Value
AMPK ()
CaM-KKβ (Cell-free assay)	47 nM(Ki)
CaM-KKα (Cell-free assay)	0.25 μM(Ki)

STO-609抑制重组CaM-KKα和CaM-KKβ的活性，Ki值分别为80 ng/ml和15 ng/ml，STO-609还抑制它们的自身磷酸化活性。STO-609对CaM-KK具有高度选择性，对其下游 CaM激酶(CaM-KI and -IV)没有显著作用。在转染的Hela细胞中，STO-609以剂量依赖方式抑制Ca。

对成年小鼠体内给药，STO-609会引起造骨细胞的增多、破骨细胞的减少，对卵巢切除术引发的骨质疏松症具有保护作用。脑室注射STO-609不影响对神经低血糖症的负调节反应、对低血糖引起的AMPK激活也没有影响。