Marizomib (Salinosporamide A) 是第二代不可逆的脑渗透性泛蛋白酶体(proteasome)抑制剂。Marizomib 抑制 20S 蛋白酶体的 CT-L (β5)、CT-T-laspase 样 (C-L, β1) 和胰蛋白酶样 (T-L, β2) 活性 (IC50分别为 3.5, 28, 430 nM)。
| 生物活性 | Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant,pan-proteasomeinhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20Sproteasome(IC50=3.5, 28, and 430 nM, respectively)[1][2][3]. |
| IC50& Target | IC50: 3.5 nM (CT-L), 28 nM (CT-T-laspase-like), 430 nM (trypsin-like)[1] |
体外研究
(In Vitro) | Marizomib (Salinosporamide A) (0.1-10000 nM; 72 hours) effectively reduces survival of D-54 and U-251 cells in a dose-dependent manner. The IC50s are ~52 nM for U-251 and ~20 nM for D-54[1].
Marizomib (24 hours; 60 nM) induces apoptosis and caspase-3 activation in glioma cells[1].
Cell Proliferation Assay[1] | Cell Line: | U-251 and D-54 cells | | Concentration: | 0.1, 1, 10, 100, 1000, 10000 nM | | Incubation Time: | 72 hours | | Result: | Effectively reduced survival of D-54 and U-251 cells in a dose-dependent manner. |
Apoptosis Analysis[1] | Cell Line: | D-54 cells | | Concentration: | 60 nM | | Incubation Time: | 24 hours | | Result: | Induces D-54 cells apoptosis. |
Western Blot Analysis[1] | Cell Line: | D-54 cells | | Concentration: | 60 nM | | Incubation Time: | 24 hours | | Result: | Led to increased activity of caspase-3 in a dose-dependent manner. |
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体内研究
(In Vivo) | Marizomib (Salinosporamide A) (0.15 mg/kg; i.v; twice a week for three weeks) significantly decreases tumor growth, and is not associated with any toxicity[3].
| Animal Model: | CB-17 SCID-male mice (4-6 weeks old)[3] | | Dosage: | 0.15 mg/kg | | Administration: | i.v; twice a week for three weeks | | Result: | Significantly decreased tumor growth, and was not associated with any toxicity. |
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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 : ≥ 100 mg/mL(318.69 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.1869 mL | 15.9347 mL | 31.8695 mL | | 5 mM | 0.6374 mL | 3.1869 mL | 6.3739 mL | | 10 mM | 0.3187 mL | 1.5935 mL | 3.1869 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 (6.63 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.63 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%corn oil Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.63 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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