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• 产品描述： (-)-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

• 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. (-)-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 (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. (-)-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. Cell Proliferation Assay 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 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 Cell Line: MT-1 cells Concentration: 10 μg/

• 体内研究：
  (-)-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. Animal Model: Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells 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.

• 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. Int J Mol Sci. 2018 Mar 3;19(3):729. 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.828 ml	19.14 ml	38.28 ml
  5 mM	0.766 ml	3.828 ml	7.656 ml
  10 mM	0.383 ml	1.914 ml	3.828 ml
  50 mM	0.077 ml	0.383 ml	0.766 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *