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。
生物活性 | CKI-7 free base is a potent and ATP-competitivecasein kinase1 (CK1)inhibitor with anIC50of 6 μM and aKiof 8.5 μM. CKI-7 free base is a selectiveCdc7 kinaseinhibitor. CKI-7 free base also inhibitsSGK,ribosomal S6 kinase-1 (S6K1)andmitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect oncasein kinaseII and other protein kinases[1][2][3][4]. |
IC50& Target[1][2][3] | CK1 6 μM (IC50) | CK1 8.5 μM (Ki) | Cdc7 | SGK | MSK1 |
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体外研究 (In Vitro) | 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[1]. 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[1].
RT-PCR[1] 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[1] Cell Line: | Mouse ES cells | Concentration: | 5 μM | Incubation Time: | 5 days | Result: | Suppressed SFEB-induced β-catenin stabilization on day 5. |
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体内研究 (In Vivo) | 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[2].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 25 mg/mL(87.49 mM;Need ultrasonic) 配制储备液 1 mM | 3.4996 mL | 17.4978 mL | 34.9956 mL | 5 mM | 0.6999 mL | 3.4996 mL | 6.9991 mL | 10 mM | 0.3500 mL | 1.7498 mL | 3.4996 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (7.28 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.28 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (7.28 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.28 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (7.28 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.28 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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