中文名称: | (-)-DHMEQ | ||||
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英文名称: | (-)-DHMEQ | ||||
别名: | 2-羟基-n-((1s,2s,6s)-2-羟基-5-氧代-7-噁双环[4.1.0]-3-庚烯-3-基)苯甲酰胺 Dehydroxymethylepoxyquinomicin | ||||
CAS No: | 287194-40-5 | 分子式: | C13H11NO5 | 分子量: | 261.23 |
CAS No: | 287194-40-5 | ||||
分子式: | C13H11NO5 | ||||
分子量: | 261.23 |
基本信息
产品编号: |
D11527 |
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产品名称: |
(-)-DHMEQ |
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CAS: |
287194-40-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃(储于氮气) |
6个月 |
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分子量: |
261.23 |
-20℃(储于氮气) |
1个月 |
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化学名: |
Dehydroxymethylepoxyquinomicin |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
3.8280mL |
19.1402mL |
38.2804mL |
5mM |
0.7656mL |
3.8280mL |
7.6561mL |
10mM |
0.3828mL |
1.9140mL |
3.8280mL |
生物活性
产品描述 |
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。 |
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靶点 |
RelA |
RelB |
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体外研究 |
(-)-DHMEQ (Dehydroxymethylepoxyquinomicin;2-10μg/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 (10μg/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 (10μg/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 DNAbinding of RelB,but also its interaction to importin.(-)-DHMEQ also induces instability of RelB. Cell Proliferation Assay |
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Cell Line: |
TL-Om1,MT-1,KK-1,ST-1 and K562 cells |
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Concentration: |
2μg/mL,5μg/mL,10μg/mL |
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Incubation Time: |
12 hours,24 hours,48 hours |
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Result: |
Significantly reduced the viability of all cell lines in a dose- and time-dependent manner. |
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Apoptosis Analysis |
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Cell Line: |
TL-Om1,MT-1 and K562 cells |
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Concentration: |
10μg/mL |
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Incubation Time: |
0 hours,24 hours,48 hours |
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Result: |
Annexin V-positive cells were significantly increased after 24 to 48 hours. |
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Western Blot Analysis |
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Cell Line: |
MT-1 cells |
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Concentration: |
10μg/mL |
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Incubation Time: |
4 hours,8 hours,16 hours |
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Result: |
Annexin V-positive cells were significantly increased after 24 to 48 hours. |
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体内研究 |
(-)-DHMEQ (Dehydroxymethylepoxyquinomicin;4mg/kg or 12mg/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. |
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Animal Model: |
Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells |
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Dosage: |
4mg/kg or 12mg/kg |
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Administration: |
Intraperitoneal injection;on day 0 and 3 times a week;for one month |
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Result: |
Showed a significant increase in the survival rate in mice. |
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 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )