生物活性 | HOIPIN-8 is a potent inhibitor oflinear ubiquitin chain assembly complex (LUBAC)with anIC50of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediatedNF-κBactivation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC[1]. | ||||||||||||||||
体外研究 (In Vitro) | HOIPIN-8 (0-100 μM; 72 hours) has little cell toxicity on A549 cells, and exhibits an IC50value of 100 μM[1].HOIPIN-8 (0-10 μM; 24 hours) has an inhibitory effect over 10-fold enhancement over that of HOIPIN-1 on NF-κB activation, exhibits an IC50value of 0.42 μM in HEK293T cells[1].HOIPIN-8 (0-30 μM; NF-κB luciferase reporter is transfected into cells for 18 hours; then with 10 ng/ml TNF-α for 6 h) exhibits a 4-fold enhancements of the potency than HOIPIN-1, the IC50value is 11.9 μM. It also effectively reduces IL-1β-induced expression of NF-κB target genes, such as ICAM1 and IL-6 as compared to HOIPIN-1[1]. Cell Viability Assay[1]
RT-PCR[1]
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分子量 | 456.38 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C23H15F2N4NaO3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | -20°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) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 100 mg/mL(219.12 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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