CKI-7

生物活性靶点体外研究体内研究 CKI-7 试剂级价格

CKI-7

CAS号:120615-25-0
英文名:CKI-7
中文名:CKI-7
CBNumber:CB4503226
分子式:C11H12ClN3O2S
分子量:285.75
MOL File:120615-25-0.mol

CKI-7化学性质

熔点 :188-190°C
沸点 :499.7±55.0 °C(Predicted)
密度 :1.432±0.06 g/cm3(Predicted)
储存条件 :−20°C
溶解度 :H₂O: 9 mg/mL
形态 :solid
酸度系数(pKa) :7.80±0.50(Predicted)
颜色 :white

安全信息

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/PG 3
WGK Germany :3
海关编码 :2933499090

CKI-7性质、用途与生产工艺

生物活性 CKI-7 free base 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 free base 选择性抑制 Cdc7 激酶，还抑制 SGK，S6K1 以及 MSK1。CKI-7 free base 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.