STO-609

生物活性靶点体外研究体内研究 STO-609 试剂级价格

STO-609

CAS号:52029-86-4
英文名:7-OXO-7H-BENZIMIDAZO[2,1-A]BENZ[DE]ISOQUINOLINE-3-CARBOXYLIC ACID ACETATE
中文名:STO-609
CBNumber:CB6245603
分子式:C19H10N2O3
分子量:314.29
MOL File:52029-86-4.mol

STO-609化学性质

熔点 :>300 °C
沸点 :716.9±62.0 °C(Predicted)
密度 :1.54±0.1 g/cm3(Predicted)
储存条件 :Sealed in dry,2-8°C
溶解度 :DMSO: 15 mg/mL at ≥60 °C
形态 :solid
酸度系数(pKa) :2.65±0.20(Predicted)

安全信息

安全说明 :22-24/25
WGK Germany :3

STO-609性质、用途与生产工艺

生物活性 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。
靶点
Target Value
AMPK
()
CaM-KKβ
(Cell-free assay) 47 nM(Ki)
CaM-KKα
(Cell-free assay) 0.25 μM(Ki)
体外研究

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。
体内研究
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。
用途一种特异性的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.