CLZ-8 (Compound 8) 是具有口服活性的Mcl-1-PUMA的抑制剂，Ki值为 0.3 μM。CLZ-8 在下调 PUMA 依赖的凋亡（apoptosis）的同时还能抑制 Mcl-1 介导的癌细胞抗凋亡作用。
| 生物活性 | CLZ-8 (Compound 8) is an orally activeMcl-1-PUMAinterface inhibitor, with aKiof 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependentapoptosiswhile deactivating Mcl-1-mediated anti-apoptosis incancercells[1]. |
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体外研究
(In Vitro) | CLZ-8 (Compound 8) (0-160 μM, 48 h) significantly inhibits PUMA-dependent apoptosis[1].
CLZ-8 (0-1 μM, 2 h) significantly enhance the irradiated cell viability in a dose-dependent manner, provides significant protection for HUVECs, and inhibits overexpressed PUMA[2].
CLZ-8 (0-1 μM, 24 h) attenuates the radiation-induced apoptosis[2].
CLZ-8 (1 μM, 2 h) protects HUVECs from DNA breaks[2].
Apoptosis Analysis[1][2] | Cell Line: | DLD-1 cells or HUVEC cells | | Concentration: | 0-160 μM (DLD-1) or 0.01, 0.1 and 1 μM (HUVECs) | | Incubation Time: | 48 h (DLD-1) or 24 h (HUVECs) | | Result: | Significantly inhibited PUMA-dependent apoptosis with an IC50of 38.93 ± 0.91 μM.
Attenuated the radiation-induced apoptosis. |
Western Blot Analysis[2] | Cell Line: | HUVEC cells | | Concentration: | 0.001, 0.01, 0.1 and 1 μM | | Incubation Time: | 2 h | | Result: | Suppressed induction of PUMA after radiation, significantly decreased the level of p53.
Significantly decreased the level of MCL-1 and increased the level of Bcl-XL. |
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体内研究
(In Vivo) | CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice[2].
| Animal Model: | 6-8 week-old male BALB/c mice[2] | | Dosage: | 100, 200 and 400 mg/kg | | Administration: | Intragastric administration, once, 30 min prior to irradiation | | Result: | Increased the survival rate of irradiated mice. |
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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 : 50 mg/mL(127.06 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.5413 mL | 12.7065 mL | 25.4130 mL | | 5 mM | 0.5083 mL | 2.5413 mL | 5.0826 mL | | 10 mM | 0.2541 mL | 1.2706 mL | 2.5413 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 90%corn oil Solubility: ≥ 0.83 mg/mL (2.11 mM); Clear solution
此方案可获得 ≥ 0.83 mg/mL (2.11 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 8.3 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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