52029-86-4
中文名稱
STO-609
英文名稱
7-OXO-7H-BENZIMIDAZO[2,1-A]BENZ[DE]ISOQUINOLINE-3-CARBOXYLIC ACID ACETATE
CAS
52029-86-4
分子式
C19H10N2O3
分子量
314.29
MOL 文件
52029-86-4.mol
更新日期
2025/01/09 18:04:24
52029-86-4 結(jié)構(gòu)式
基本信息
中文別名
化合物STO609 英文別名
STO-609STO-609, >98%
STO609
STO 609
STO-609 ACETATE
STO-609 free base
STO-609 ACETIC ACID
STO-609 - CAS 52029-86-4 - Calbiochem
7-Oxo-7H-benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic Acid
7H-Benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic acid, 7-oxo-
7-OXO-7H-BENZIMIDAZO[2,1-A]BENZ[DE]ISOQUINOLINE-3-CARBOXYLIC ACID ACETATE
所屬類別
生物化工:激動劑抑制劑物理化學(xué)性質(zhì)
熔點(diǎn)>300 °C
沸點(diǎn)716.9±62.0 °C(Predicted)
密度1.54±0.1 g/cm3(Predicted)
儲存條件Sealed in dry,2-8°C
溶解度DMSO: 15 mg/mL at ≥60 °C
酸度系數(shù)(pKa)2.65±0.20(Predicted)
形態(tài)solid
顏色Light yellow to yellow
應(yīng)用領(lǐng)域
用途1
一種特異性的CaM-KK的抑制劑,抑制CaM-KKα和CaM-KKβ,Ki值分別為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價格(試劑級)
報(bào)價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-19805 | STO-609 STO-609 | 52029-86-4 | 1mg | 400元 |
2024/11/08 | HY-19805 | STO-609 STO-609 | 52029-86-4 | 5mg | 800元 |
2024/11/08 | HY-19805 | STO-609 STO-609 | 52029-86-4 | 10mg | 1280元 |
常見問題列表
生物活性
STO-609 是特異性的CaM-KK的抑制劑,抑制CaM-KKα和CaM-KKβ的活性,Ki值分別為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。靶點(diǎn)
Target | Value |
AMPK
() | |
CaM-KKβ
(Cell-free assay) | 47 nM(Ki) |
CaM-KKα
(Cell-free assay) | 0.25 μM(Ki) |
體外研究
STO-609抑制重組CaM-KKα和CaM-KKβ的活性,Ki值分別為80 ng/ml和15 ng/ml,STO-609還抑制它們的自身磷酸化活性。STO-609對CaM-KK具有高度選擇性,對其下游 CaM激酶(CaM-KI and -IV)沒有顯著作用。在轉(zhuǎn)染的Hela細(xì)胞中,STO-609以劑量依賴方式抑制Ca。
體內(nèi)研究
對成年小鼠體內(nèi)給藥,STO-609會引起造骨細(xì)胞的增多、破骨細(xì)胞的減少,對卵巢切除術(shù)引發(fā)的骨質(zhì)疏松癥具有保護(hù)作用。腦室注射STO-609不影響對神經(jīng)低血糖癥的負(fù)調(diào)節(jié)反應(yīng)、對低血糖引起的AMPK激活也沒有影響。