CKI-7

CKI-7用途

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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CKI-7名称

[ CAS 号 ]:
1177141-67-1

[ 英文名 ]:
CKI-7 HCl

[英文别名 ]:

CKI-7 dihydrochloride

CKI-7生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> SGK

信号通路 >> 细胞周期/DNA损伤 >> CDK

信号通路 >> 细胞周期/DNA损伤 >> 酪蛋白激酶

信号通路 >> MAPK/ERK信号通路 >> 核糖体S6激酶(RSK)

信号通路 >> 干细胞及 Wnt 通路 >> 酪蛋白激酶

[ 靶点 ]

CK1:6 μM (IC50)

CK1:8.5 μM (Ki)

Cdc7

SGK

S6K1

MSK1

[体外研究]

CKI-7(0.1-10μM；5天；ES细胞)治疗显著增加早期神经外胚层标记物Sox1的表达以及神经标记物nestin和βIII微管蛋白阳性的细胞数量,呈浓度依赖性[1]。CKI-7(5μM；5天；ES细胞)治疗在第5天抑制SFEB诱导的β-catenin稳定,表明CKI-7抑制Wnt信号传导[1]。RT-PCR[1]细胞系：小鼠ES细胞浓度：0.1-10μM孵育时间：5d。结果：早期神经外胚层标志物Sox1的表达显著增加,神经标志物nestin和βIII微管蛋白阳性细胞数明显增加。westernblot分析[1]细胞系：小鼠ES细胞浓度：5μM孵育时间：5d结果：抑制SFEB诱导的β-catenin稳定。

[体内研究]

利用新近分离的费城染色体阳性急性淋巴细胞白血病细胞系,在SCID米色小鼠全身性肿瘤模型上证明了CKI-7具有剂量依赖性的抗肿瘤活性。标准细胞周期同步研究证实,暴露于CKI-7导致细胞周期依赖性caspase3激活和凋亡细胞死亡[2]。

[参考文献]

[1]. Osakada F, et al. In vitro differentiation of retinal cells from human pluripotent stem cells by small-molecule induction. J Cell Sci. 2009 Sep 1;122(Pt 17):3169-79.

[2]. Mark G. Frattini, et al. Small Molecule Inhibition of Cdc7, a Key Cell Cycle Regulator and Novel Therapeutic Target, Successfully Inhibits Leukemia Cell Growth in Vitro and in Vivo. Blood (2008) 112 (11): 2668.

[3]. Chijiwa T, et al. A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis. J Biol Chem. 1989 Mar 25;264(9):4924-7.

[4]. Rena G, et al. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO Rep. 2004 Jan;5(1):60-5.

CKI-7物理化学性质

[ 分子式 ]:
C₁₁H₁₄Cl₃N₃O₂S

[ 分子量 ]:
358.67200

[ 精确质量 ]:
356.98700

[ PSA ]:
93.46000

[ LogP ]:
4.90120

[ 外观性状 ]:
白色-浅褐色固体

[ 储存条件 ]:
-20°C

CKI-7MSDS

详细MSDS(安全技术说明书)

CKI-7安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T+

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

[ 危险类别 ]:
6.1

CKI-7文献

An update on metabolic assessment in patients with urinary lithiasis.

World J. Urol. , (2014)

The objective of this study was to evaluate the prevalence of urinary metabolic abnormalities in patients with urolithiasis and their potential risk factors.A total of 905 stone patients were evaluate...

Clinical characteristics and outcome of 467 patients with a clinically recognized eating disorder identified among 52,215 patients with type 1 diabetes: a multicenter german/austrian study.

Diabetes Care , (2014)

To compare clinical characteristics and outcome of type 1 diabetes mellitus (T1DM) between patients with and without a clinically recognized eating disorder (ED).A total of 52,215 T1DM patients aged 8...

Uterine adenomyosis and in vitro fertilization outcome: a systematic review and meta-analysis.

Hum. Reprod. , (2014)

Is adenomyosis associated with IVF/ICSI outcome in terms of clinical pregnancy rate?In a meta-analysis of published data, women with adenomyosis had a 28% reduction in the likelihood of clinical pregn...

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