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HOIPIN-1 (Synonyms: JTP-0819958) 纯度: 97.10%
HOIPIN-1 (JTP-0819958) 是一种选择性线性泛素链组装复合物 (LUBAC) 抑制剂,IC50 值 >2.8 μM。HOIPIN-1 抑制 LUBAC 介导的 NF-kB 激活。
HOIPIN-1 Chemical Structure
规格 | 价格 | 是否有货 | 数量 |
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5 mg | ¥700 | In-stock | |
10 mg | ¥1200 | In-stock | |
25 mg | ¥2500 | In-stock | |
50 mg | ¥4000 | In-stock | |
100 mg | ¥6000 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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HOIPIN-1 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Immunology/Inflammation Compound Library
- Kinase Inhibitor Library
- NF-κB Signaling Compound Library
- Stem Cell Signaling Compound Library
- Anti-Cancer Compound Library
- Anti-Aging Compound Library
- Differentiation Inducing Compound Library
- Pyroptosis Compound Library
- Targeted Diversity Library
- Anti-Liver Cancer Compound Library
生物活性 |
HOIPIN-1 (JTP-0819958) is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM[1]. HOIPIN-1 suppress LUBAC-mediated NF-kB activation in vitro[2]. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
In the HTRF-based LUBAC-mediated ubiquitination assay with Petit-LUBAC. HOIPIN-1 (0.9-120 μM) exhibits an increased inhibitory activity with a a longer preincubation time in the reaction buffer. The IC50 values are 26 μM, 26 μM, 26 μM, and 3.926 μM, at 1h, 3h, 6h and 24 h, respectively[1].The coexpression of the LUBAC subunits in HEK293T cells increases the intracellular amounts of linear polyubiquitin, HOIPIN-1 (1-30 μM) dose dependently suppressed the production of intracellular linear polyubiquitin in LUBAC-expressing HEK293T cells[1].HOIPIN-1 (30-100 μM; 30-60 mins) inhibits IL-1β-induced NF-κB activation and decreases the phosphorylation of IKKα/β, p105, and p65 in hela cells[1].HOIPIN-1 (10-100 μM) inhibits the expression of NF-κB target genes such as ICAM1 and TNF-α in IL-1β-induced hela cells in a dose-dependent manner[1].The linear ubiquitin chain assembly complex (LUBAC), composed of the HOIL-1L, HOIP, and SHARPIN subunits. HOIPIN-1 exhibits IC50 values of 4.4 μM, 3.5 μM and 3.7 μM for inhibition of linear polyubiquitination activity by the HOIL-1L/HOIP complex, the HOIL-1L/HOIP/SHARPIN complex and the HOIP/SHARPIN complex, respectively[2].HOIPIN-1 (1-100 μM; 72 hours) shows no apparent cytotoxicity based on ATP content, it exhibits cytotoxicity in A549 cells with an IC50>100 μM in A549 cells[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
304.27 |
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Formula |
C17H13NaO4 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
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溶解性数据 |
In Vitro:
DMSO : 5 mg/mL (16.43 mM; Need ultrasonic) 配制储备液
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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。 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
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参考文献 |
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