(-)-DHMEQ  ≥98%

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包装规格:2mg 5mg 10mg 25mg in glass bottle
产品简介:一种有效,选择性且不可逆的NF-κB抑制剂,与半胱氨酸残基共价结合。(-)-DHMEQ抑制NF-κB的核易位,并显示抗炎和抗癌活性。
溶解性:溶于DMSO(≥30mg/mL)
储备液保存:-80°C, 6 months -20°C, 1 month (stored under nitrogen)
体内实验:1、请依序添加每种溶剂: 10% DMSO→40% PEG300→5% Tween-80→45% Saline Solubility: 5 mg/mL (19.14 mM); 悬浊液; 超声助溶 此方案可获得 5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL。 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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。
靶点:RelA;RelB
体外研究:(-)-DHMEQ (Dehydroxymethylepoxyquinomicin; 2-10 μg/mL; 12-48 hours) treatment significantly reduces the viability of all cell lines in a dose- and time-dependent manner, whereas the effect is not significant in a control cell line K562 without constitutive NF-κB activity.v (-)-DHMEQ (10 μg/mL; 0-48 hours; TL-Om1, MT-1 and K562 cells) treatment significantly increases the Annexin V-positive cells in MT-1 and TL-Om1 cell lines. (-)-DHMEQ (10μg/mL;4-16 hours; MT-1 cells) treatment down-regulates Bcl-xL, Bcl-2, c-myc, cyclin D1, Rb, and p53, and up-regulates proapoptotic genes such as caspase-3, -8, and-9. (-)-DHMEQ treatment increases cells in G0 /G1 phase in a time-dependent manner, demonstrating antiproliferative effects of (-)-DHMEQ. (-)-DHMEQ binds to p65, cRel, RelB, and p50, but not to p52 at specific cysteine residues. (-)-DHMEQ inhibits not only DNA-binding of RelB, but also its interaction to importin. (-)-DHMEQ also induces instability of RelB.
体内研究:(-)-DHMEQ (4 mg/kg or 12 mg/kg; intraperitoneal injection; on day 0 and 3 times a week; for one month; SCID mice) treatment shows a significant increase in the survival rate in mice.
保存条件:-20℃
注意事项:1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。