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1177141-67-1

中文名称 CKI-7 DIHYDROCHLORIDE
英文名称 N-(2-Aminoethyl)-5-chloroisoquinoline-8-sulfonamide Dihydrochloride
CAS 1177141-67-1
分子式 C11H14Cl3N3O2S
分子量 358.672
MOL 文件 1177141-67-1.mol
1177141-67-1 结构式 1177141-67-1 结构式

基本信息

中文别名
CKI-7 二盐酸盐
N-(2-氨基乙基)-5-氯异喹啉-8-磺酰胺二盐酸盐
英文别名
CKI-7 dihydrochlorid
CKI-7 Dihydrochloride
N-(2-Aminoethyl)-5-chloroisoquinoline-8-sulfonamide Dihydrochloride

物理化学性质

熔点187-189°C
储存条件-20°C
储存条件-20°C冷冻
溶解度在水中的溶解度>5mg/mL
形态固体
颜色白色至浅棕褐色

安全数据

危险性符号(GHS)
GHS06
警示词危险
危险性描述H301
防范说明P301+P310
危险品标志T
危险类别码25
安全说明45
危险品运输编号UN 2811 6.1 / PGIII
WGK Germany3

常见问题列表

生物活性
CKI-7 是一种有效且 ATP 竞争性的酪蛋白激酶 1 (CK1) 抑制剂,IC50 为 6 μM,Ki 为 8.5 μM。CKI-7 选择性抑制 Cdc7 激酶,还抑制 SGK,S6K1 以及 MSK1。CKI-7 对酪蛋白激酶 II 和其他蛋白激酶的作用弱得多。
靶点

CK1

6 μM (IC 50 )

CK1

8.5 μM (Ki)

Cdc7

SGK

S6K1

MSK1

体外研究

CKI-7 (0.1-10 μM; 5 days; ES cells) treatment significantly increases the expression of the early neuroectodermal marker Sox1 and the number of cells positive for the neural markers nestin and βIII-tubulin, in a concentration-dependent manner.
CKI-7 (5 μM; 5 days; ES cells) treatment suppresses SFEB-induced β-catenin stabilization on day 5, indicating that CKI-7 inhibits Wnt signaling.

RT-PCR

Cell Line: Mouse ES cells
Concentration: 0.1-10 μM
Incubation Time: 5 days
Result: Significantly increased the expression of the early neuroectodermal marker Sox1 and the number of cells positive for the neural markers nestin and βIII-tubulin, in a concentration-dependent manner.

Western Blot Analysis

Cell Line: Mouse ES cells
Concentration: 5 μM
Incubation Time: 5 days
Result: Suppressed SFEB-induced β-catenin stabilization on day 5.
体内研究

In vivo dose-dependent anti-tumor activity of CKI-7 is demonstrated in a SCID-Beige mouse systemic tumor model utilzing a recently isolated Philadelphia chromosome positive acute lymphoblastic leukemia cell line. Standard cell cycle synchronization studies established that exposure to CKI-7 results in cell cycle dependent caspase 3 activation and apoptotic cell death.

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