中文名 | (-)-DHMEQ |
英文名 | (-)-DHMEQ |
别名 | 化合物 T11018L NF-ΚB抑制剂((+)-DHMEQ) 2-羟基-N-(((1S,2S,6S)-2-羟基-5-氧代-7-氧杂双环[4.1.0]庚-3-烯-3-基)苯甲酰胺 |
英文别名 | DHMEQ DHM2EQ (-)-DHMEQ 287194-40-5 DEHYDROXYMETHYLEPOXYQUINOMICIN Dehydroxymethylepoxyquinomicin (DHMEQ) (-)-DHMEQ?(dehydroxymethylepoxyquinomicin) 2-hydroxy-N-[(1S,2S,6S)-2-hydroxy-5-oxo-7-oxabicyclo[4.1.0]hept-3-en-3-yl]benzaMide Benzamide, 2-hydroxy-N-[(1S,2S,6S)-2-hydroxy-5-oxo-7-oxabicyclo[4.1.0]hept-3-en-3-yl]- |
CAS | 287194-40-5 |
化学式 | C13H11NO5 |
分子量 | 261.23 |
溶解度 | DMSO: ≥ 32 mg/mL |
存储条件 | -20℃ |
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/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 | (-)-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. |
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 |
5 mM | 0.077 ml | 0.383 ml | 0.766 ml |
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