(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) 是一种有效，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。
| 生物活性 | (-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversibleNF-κBinhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation ofNF-κBand shows anti-inflammatory and anticancer activity[1][2][3]. |
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体外研究
(In Vitro) | (-)-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[2].
(-)-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[2].
(-)-DHMEQ (10 μg/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[2].
(-)-DHMEQ treatment increases cells in G0 /G1 phase in a time-dependent manner, demonstrating antiproliferative effects of (-)-DHMEQ[2].
(-)-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[1].
Cell Proliferation Assay[2] | Cell Line: | TL-Om1, MT-1, KK-1, ST-1 and K562 cells | | Concentration: | 2 μg/mL, 5 μg/mL, 10 μg/mL | | Incubation Time: | 12 hours, 24 hours, 48 hours | | Result: | Significantly reduced the viability of all cell lines in a dose- and time-dependent manner. |
Apoptosis Analysis[2] | Cell Line: | TL-Om1, MT-1 and K562 cells | | Concentration: | 10 μg/mL | | Incubation Time: | 0 hours, 24 hours, 48 hours | | Result: | Annexin V-positive cells were significantly increased after 24 to 48 hours. |
Western Blot Analysis[2] | Cell Line: | MT-1 cells | | Concentration: | 10 μg/mL | | Incubation Time: | 4 hours, 8 hours, 16 hours | | Result: | Annexin V-positive cells were significantly increased after 24 to 48 hours. |
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体内研究
(In Vivo) | (-)-DHMEQ (Dehydroxymethylepoxyquinomicin; 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[2].
| Animal Model: | Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells[2] | | Dosage: | 4 mg/kg or 12 mg/kg | | Administration: | Intraperitoneal injection; on day 0 and 3 times a week; for one month | | Result: | Showed a significant increase in the survival rate in mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(191.40 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.8280 mL | 19.1402 mL | 38.2804 mL | | 5 mM | 0.7656 mL | 3.8280 mL | 7.6561 mL | | 10 mM | 0.3828 mL | 1.9140 mL | 3.8280 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 (stored under nitrogen)。-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: 5 mg/mL (19.14 mM); Suspended solution; Need ultrasonic
此方案可获得 5 mg/mL (19.14 mM) 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；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。 *以上所有助溶剂都可在本网站选购。
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