WEHI-345 是一种有效的选择性RIPK2 激酶抑制剂，IC50值为 0.13 μM。WEHI-345 在寡聚化结构域 (NOD) 刺激下可延迟RIPK2的泛素化和NF-κB的活化。
| 生物活性 | WEHI-345 is a potent and selectiveRIPK2kinaseinhibitor with anIC50of 0.13 μM, which delaysRIPK2ubiquitylation andNF-κBactivation on oligomerization domain (NOD) stimulation[1]. |
| IC50& Target | IC50: 0.13 μM (RIPK2 kinase)[1] |
体外研究
(In Vitro) | WEHI-345 (500 nM; Raw 267.4 cells) is able to inhibit MDP-induced autophosphorylation activity of RIPK2 in cells[1].
WEHI-345 (500 nM; 0 hour, 2 hours, 4 hours, 8 hours; BMDMs or THP-1 cells) potently blocks MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in bone marrow-derived macrophages (BMDMs). In THP-1 cells, WEHI-345 reduces mRNA levels of NF-kB targets such as TNF, IL-8, IL-1b and A20[1].
Western Blot Analysis[1] | Cell Line: | Raw 267.4 cells | | Concentration: | 500 nM | | Incubation Time: | | | Result: | Inhibited MDP-induced autophosphorylation activity of RIPK2 in cells. |
RT-PCR[1] | Cell Line: | BMDMs or THP-1 cells | | Concentration: | 500 nM | | Incubation Time: | 0 hour, 2 hours, 4 hours, 8 hours | | Result: | Blocked MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in BMDMs. And reduced mRNA levels of NF-kB targets in THP-1 cells. |
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体内研究
(In Vivo) | WEHI-345 (20 mg/kg; intraperitoneal injection; twice daily; for 6 days; C57BL/6 male mice) treatment reduces disease score, inflammatory infiltrate, histological score and recruitment of dendritic cells to the site of inflammation. And improves body weight and reduces cytokine and chemokine levels, indicating an overall improvement of the condition in experimental autoimmune encephalomyelitis (EAE)-induced wild-type C57Bl/6 mice[1].
| Animal Model: | C57BL/6 male mice (8-week-old)[1] | | Dosage: | 20 mg/kg | | Administration: | Intraperitoneal injection; twice daily; for 6 days | | Result: | Reduced disease score, inflammatory infiltrate, histological score and recruitment of dendritic cells to the site of inflammation. And improved body weight and reduced cytokine and chemokine levels. |
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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(62.27 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.4909 mL | 12.4545 mL | 24.9091 mL | | 5 mM | 0.4982 mL | 2.4909 mL | 4.9818 mL | | 10 mM | 0.2491 mL | 1.2455 mL | 2.4909 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% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.23 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.23 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 25.0 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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