287194-40-5
基本信息
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
DHM2EQ
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]-
物理化学性质
| 熔点 | 187 °C |
| 沸点 | 617.2±55.0 °C(Predicted) |
| 密度 | 1.58±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | DMSO : ≥ 32 mg/mL (122.50 mM) |
| 酸度系数(pKa) | 8.43±0.30(Predicted) |
| 形态 | Solid |
| 颜色 | Off-white to gray |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P305+P351+P338 |
常见问题列表
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RelA
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RelB
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(-)-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. |
(-)-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. |