CKI-7 DIHYDROCHLORIDE
- CAS号:1177141-67-1
- 英文名:N-(2-Aminoethyl)-5-chloroisoquinoline-8-sulfonamide Dihydrochloride
- 中文名:CKI-7 DIHYDROCHLORIDE
- CBNumber:CB31176497
- 分子式:C11H14Cl3N3O2S
- 分子量:358.67176
- MOL File:1177141-67-1.mol
- 熔点 :187-189°C
- 储存条件 :-20°C
- 溶解度 :H2O: >5mg/mL
- 形态 :solid
- 颜色 :white to light tan
CKI-7 DIHYDROCHLORIDE性质、用途与生产工艺
- 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。
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靶点
CK1
6 μM (IC 50 )
CK1
8.5 μM (Ki)
Cdc7
SGK
S6K1
MSK1
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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.
- 公司名称:TORONTO
- 联系电话:--
- 电子邮件:info@trc-canada.com
- 国家:加拿大
- 产品数:6038
- 优势度:71