| 1-Naphthyl 3,5-dinitrobenzoatedual 5-lipoxygenase and microsomal prostaglandin E synthase-1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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| Cas No. | 93261-39-3 | SDF | Download SDF |
| Synonyms | 1-(3,5-Dinitrobenzoyloxy)naphthalene,1-Naphthalonol 3,5-dinitrobenzoate | ||
| Chemical Name | 1-(3,5-dinitrobenzoate) 1-naphthalenol | ||
| Canonical SMILES | O=C(C1=CC([N+]([O-])=O)=CC([N+]([O-])=O)=C1)OC2=CC=CC3=C2C=CC=C3 | ||
| Formula | C17H10N2O6 | M.Wt | 338.3 |
| Solubility | ≤0.1mg/ml in methanol;0.5mg/ml in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 1 and 3.6 μM for 5-lipoxygenase and microsomal prostaglandin E synthase-1, respectively
1-Naphthyl 3,5-dinitrobenzoate is a dual 5-lipoxygenase and microsomal prostaglandin E synthase-1 inhibitor.
Human 5-lipoxygenase (5-LOX), a target for antiinflammation drug design, catalyzes the first two reactions in the production of leukotrienes from arachidonic acid (AA): oxygenation of AA to 5-HPETE and further dehydration to leukotriene A4 (LTA4). Then LTA4 is metabolized to other leukotrienes. Furthermore, 5-LOX is also found to play key roles in tumor formation and cancer metastasis and thus is considered as a potential target for anticancer drugs.
In vitro: A previous study built a comparative model for the human 5-LOX closed conformation and successfully used it in virtual screening. Out of around 200 000 compounds, 105 compounds were selected for experimental test. In cell-free assay, 30 compounds were found to have IC50 values less than 100 μM and 11 with IC50 values less than 10 μM. Eventually, 1-Naphthyl 3,5-dinitrobenzoate was screened out to have inhibition activity in the human whole blood assay with IC50 values less than 10 μM. 1-Naphthyl 3,5-dinitrobenzoate was also identified as efficient dualfunctional inhibitors of 5-LOX and mPGES-1 in both cell-free assay and cell-based assay. In addition, 1-Naphthyl 3,5-dinitrobenzoate was able to simultaneously suppress the production of LTB4 and PGE2 in human whole blood, and its targets was verified as 5-LOX and mPGES-1, not LTA4H, COX-1, COX-2 [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:[1] Wu, Y.,He, C.,Gao, Y., et al. Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors. Journal of Medicinal Chemistry 55, 2597-2605 (2012).
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配后是否应该分装,因为不能反复冻融?
多谢!
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【】可以这样输入，智能ABC，输入“v1”，后翻3页，就可以看见了，或用紫光拼音中文输入法，输入方括号就是粗体的中括号，实在不行请复制本公告中【】
同一管dna有的酶可以切开，比如dra1，ecoR1,Hind111
有的酶又完全不能切动，如BamH1，sac1，xba1，xho1，pst1
请问高手这是什么原因？?
感谢赐教~！
求问酶切体系为10ul,内切酶1ul,37℃水浴45min，不知道DNA产物是否完全被切开了？
所用内切酶信息如下
我做的双酶切反应，酶分别是宝生物的BamHI和XhoI，双酶切体系是：载体及目的片段分别是30ul，通用buffer4ul，XhoI、BamHI各2ul，无核酶水2ul，总体积40ul。载体和目的片段都是经37度酶切6h。载体上面这两个酶切位点的距离是6个碱基，目的片段是由pcr反应获得的，从puc19中p出来的，两端带有这两种酶的酶切位点，酶切完成后，做连接反应，体系如下：目的片段（全长1441bp）4ul，无核酶水3ul，10*T4DNA连接酶缓冲液1ul，载体1ul，T4DNA连接酶1ul，总体积10ul。16度过夜。之后摇菌送沉菌测序结果回来，送了5管一个都不对。重复实验两次还是不对！
之后改为先用BanHI单切载体，体系如下：载体17ul，酶1ul，buffer2ul，总体积20ul，30度切6小时后，Promega纯化试剂盒直接纯化，完了之后再用XhoI，37度酶切6小时，体系如上，再次用promega纯化试剂盒纯化，目的片段用双酶切体系酶切，之后做连接反应，之后铺板，挑取菌落共10个，摇菌13小时，取菌液做pcr鉴定，结果10个菌落全是引物2聚体，跑出来的条带都是100bp左右。
各位老师这是怎么回事呢？为什么连接不上呢？小弟先谢过各位大哥了！
