1-Naphthyl 3,5-dinitrobenzoate
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 338.3 |
Cas No. | 93261-39-3 |
Formula | C17H10N2O6 |
Synonyms | 1-(3,5-Dinitrobenzoyloxy)naphthalene,1-Naphthalonol 3,5-dinitrobenzoate |
Solubility | ≤0.1mg/ml in methanol;0.5mg/ml in DMSO |
Chemical Name | 1-(3,5-dinitrobenzoate) 1-naphthalenol |
SDF | Download SDF |
Canonical SMILES | O=C(C1=CC([N+]([O-])=O)=CC([N+]([O-])=O)=C1)OC2=CC=CC3=C2C=CC=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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