STO-609
中文名称 | STO-609 |
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中文同义词 | 化合物STO609;7-氧代-7H-苯并[DE]苯并[4,5]咪唑并[2,1-A]异喹啉-3-羧酸;STO609,CAM-KK 抑制剂 |
英文名称 | 7-OXO-7H-BENZIMIDAZO[2,1-A]BENZ[DE]ISOQUINOLINE-3-CARBOXYLIC ACID ACETATE |
英文同义词 | STO-609;STO-609 ACETIC ACID;7-Oxo-7H-benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic acid - acetic acid;7-Oxo-7H-benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic Acid;7H-BENZ[DE]BENZIMIDAZO[2,1-A]ISOQUINOLINE-7-ONE-3-CARBOXYLIC ACID, ACETATE;7-OXO-7H-BENZIMIDAZO[2,1-A]BENZ[DE]ISOQUINOLINE-3-CARBOXYLIC ACID ACETATE;STO-609, >98%;STO609;STO 609 |
CAS号 | 52029-86-4 |
分子式 | C19H10N2O3 |
分子量 | 314.29 |
EINECS号 | |
相关类别 | Protein Kinase |
Mol文件 | 52029-86-4.mol |
结构式 |
STO-609 性质
熔点 | >300 °C |
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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 | 在DMSO中的溶解度为15 mg/mLat ≥60 °C |
形态 | 固体 |
酸度系数(pKa) | 2.65±0.20(Predicted) |
颜色 | 浅黄至黄色 |
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。
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.安全信息
安全说明 | 22-24/25 |
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WGK Germany | 3 |
提供商 | 语言 |
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英文
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-19805 | STO-609 STO-609 | 52029-86-4 | 1mg | 400元 |
2024/08/19 | HY-19805 | STO-609 STO-609 | 52029-86-4 | 5mg | 800元 |