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(-)-DHMEQ
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(-)-DHMEQ图片
CAS NO:287194-40-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
Dehydroxymethylepoxyquinomicin
产品介绍
(-)-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].

IC50& Target[1]

RelA

 

RelB

 

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.
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.
分子量

261.23

性状

Solid

Formula

C13H11NO5

CAS 号

287194-40-5

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.8280 mL19.1402 mL38.2804 mL
5 mM0.7656 mL3.8280 mL7.6561 mL
10 mM0.3828 mL1.9140 mL3.8280 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。