(-)-DHMEQ(Synonyms: Dehydroxymethylepoxyquinomicin)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

(-)-DHMEQ (Synonyms: Dehydroxymethylepoxyquinomicin) 纯度: 98.47%

(-)-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。

(-)-DHMEQ(Synonyms: Dehydroxymethylepoxyquinomicin)

(-)-DHMEQ Chemical Structure

CAS No. : 287194-40-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2011 In-stock
2 mg ¥1400 In-stock
5 mg ¥2200 In-stock
10 mg ¥3000 In-stock
25 mg ¥6000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

(-)-DHMEQ 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Pyroptosis Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Obesity Compound Library
  • Transcription Factor Targeted Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library

生物活性

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and 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].

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.

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].

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.

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

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 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Yinzhi Lin, et al. Inhibition of Late and Early Phases of Cancer Metastasis by the NF-κB Inhibitor DHMEQ Derived from Microbial Bioactive Metabolite Epoxyquinomicin: A Review.

    [2]. Mariko Watanabe, et al. Dual targeting of transformed and untransformed HTLV-1-infected T cells by DHMEQ, a potent and selective inhibitor of NF-kappaB, as a strategy for chemoprevention and therapy of adult T-cell leukemia. Blood. 2005 Oct 1;106(7):2462-71.

    [3]. Quach HT, et al. Eudesmane-Type Sesquiterpene Lactones Inhibit Nuclear Translocation of the Nuclear Factor κB Subunit RelB in Response to a Lymphotoxin β Stimulation. Biol Pharm Bull. 2017;40(10):1669-1677.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务