B022 是一种有效的选择性的 NF-κB 诱导激酶 (NIK) 抑制剂，Ki为 4.2 nM，IC50为 15.1 nM。B022 可保护肝脏免受毒素引起的炎症，氧化应激和伤害。
| 生物活性 | B022 is a potent and selectiveNF-κB-inducing kinase (NIK)inhibitor (Kiof 4.2 nM;IC50=15.1 nM). B022 protects liver from toxin-induced inflammation, oxidative stress, and injury[1][2]. |
| IC50& Target | Ki: 4.2 nM (NF-κB-inducing kinase (NIK))[1] |
体外研究
(In Vitro) | B022 (0-5 μM; 12 hours; Hepa1 cells) treatment suppresses NIK-induced p52 formation in a dose-dependent manner[1].
B022 (0-5 μM; 12 hours; Hepa1 cells) treatment for 8 h completely blocks NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5[1].
B022 prevents NIK- or H2O2-induced β cell death and also ameliorates streptozotocin (STZ)-induced β cell death and hyperglycemia[3].
Western Blot Analysis[1] | Cell Line: | Hepa1 cells | | Concentration: | 0 μM, 0.5 μM, 5 μM | | Incubation Time: | 12 hours | | Result: | Suppressed NIK-induced p52 formation in a dose-dependent manner. |
RT-PCR[1] | Cell Line: | Hepa1 cells | | Concentration: | 0 μM, 0.5 μM, 5 μM | | Incubation Time: | 12 hours | | Result: | Dose-dependently blocked NIK-induced expression of chemokines, cytokines, and iNOS in these cells. Completely blocked NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5. |
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体内研究
(In Vivo) | B022 (30 mg/kg; intravenous injection; twice a day; for 10 days; STOP-NIK male mice) treatment inhibits NIK-triggered liver inflammation and injury in STOP-NIK mice infected with cre adenoviruses[1].
| Animal Model: | STOP-NIK male mice (8 weeks) infected with Ad-cre[1] | | Dosage: | 30 mg/kg | | Administration: | Intravenous injection; twice a day; for 10 days | | Result: | Completely prevents the lethal effect of abnormally high levels of hepatic NIK in mice. Inhibited the majority of the deteriorating effects of aberrant activation of hepatic NIK. |
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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 : 250 mg/mL(628.33 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.5133 mL | 12.5666 mL | 25.1332 mL | | 5 mM | 0.5027 mL | 2.5133 mL | 5.0266 mL | | 10 mM | 0.2513 mL | 1.2567 mL | 2.5133 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 (5.23 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.23 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 (5.23 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.23 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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