| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
LNT 1 is a potent inhibitor of flap endonuclease 1 (FEN1) with an IC50 of 46.4 nM for hFEN1-336Δ. Some sources report an IC50 of 11 nM. It binds to the active site of FEN1 and partly achieves inhibition by the coordination of Mg²⁺ ions. It shows similar potency in inhibiting exonuclease 1 (EXO1).
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| ln Vitro |
In vitro, LNT 1 is a potent FEN1 inhibitor. It binds to the active site of FEN1 and inhibits its endonuclease activity. The compound shows similar potency in inhibiting exonuclease 1 (EXO1). It is cytotoxic to SW620 colorectal cancer cells in vitro and induces a DNA damage response.
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| ln Vivo |
In vivo, LNT 1 has been shown to induce a DNA damage response and ultimately cell death. The compound's ability to inhibit FEN1, a key enzyme in DNA replication and repair, makes it a potential anticancer agent. However, detailed in vivo studies are limited. The compound is primarily used as a research tool for studying FEN1 function.
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| Enzyme Assay |
In vitro enzyme assays for LNT 1 involve measuring its ability to inhibit FEN1 endonuclease activity. Recombinant FEN1 enzyme is incubated with a fluorescently labeled flap substrate in the presence of Mg²⁺. The cleavage of the substrate is monitored by fluorescence polarization or gel electrophoresis. IC50 values are calculated from dose-response curves. The compound's ability to inhibit EXO1 is assessed using similar assays.
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| Cell Assay |
Cell-based assays for LNT 1 involve treating cancer cell lines (e.g., SW620) with the compound and assessing its effects on cell viability, DNA damage response, and cell cycle progression. Cell viability is measured by MTT or CellTiter-Glo assays. DNA damage is assessed by γ-H2AX staining and comet assays. Cell cycle analysis is performed by flow cytometry. Apoptosis is measured by caspase activation or Annexin V staining.
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| Animal Protocol |
In vivo animal studies for LNT 1 are limited. When used in animal models, the compound is typically administered to tumor-bearing mice to assess its antitumor efficacy. Tumor growth inhibition, survival, and pharmacodynamic endpoints are evaluated. However, detailed in vivo data are not widely available. The compound is primarily used as a research tool for in vitro studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of LNT 1 are not well-characterized. The compound is a small molecule with a molecular weight of 332.33 g/mol. Its absorption, distribution, metabolism, and excretion have not been extensively studied. The compound is typically used in vitro, and in vivo pharmacokinetic data are limited.
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| Toxicity/Toxicokinetics |
Toxicological profile of LNT 1 is not well-documented. The compound shows cytotoxicity to cancer cells in vitro, suggesting potential toxicity to rapidly dividing cells. As with any DNA repair inhibitor, there is a risk of off-target effects and genotoxicity. Appropriate safety precautions should be taken when handling the compound. Detailed toxicological data are not available.
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| References | |
| Additional Infomation |
LNT 1 is a research compound used to study FEN1 function and its role in DNA replication and repair. It is a valuable tool for investigating the potential of FEN1 as a therapeutic target for cancer. The compound's ability to inhibit FEN1 and induce a DNA damage response makes it a useful probe for studying DNA repair pathways. It is not approved for clinical use.
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| Molecular Formula |
C15H12N2O5S
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|---|---|
| Molecular Weight |
332.331182479858
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| Exact Mass |
332.046
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| CAS # |
824983-91-7
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| Related CAS # |
824983-91-7;
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| PubChem CID |
11652865
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| Appearance |
White to off-white solid powder
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| LogP |
1.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
504
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1N(O)C(=O)N(CC2COC3C(=CC=CC=3)O2)C2=C1SC=C2
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| InChi Key |
MXQGCMQXTPTJJT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H12N2O5S/c18-14-13-10(5-6-23-13)16(15(19)17(14)20)7-9-8-21-11-3-1-2-4-12(11)22-9/h1-6,9,20H,7-8H2
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| Chemical Name |
1-[(2,3-Dihydro-1,4-benzodioxin-2-yl)methyl]-3-hydroxythieno[3,2-d]pyrimidine-2,4(1H,3H)-dione
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| Synonyms |
LNT 1 LNT1 LNT-1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~752.26 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0091 mL | 15.0453 mL | 30.0906 mL | |
| 5 mM | 0.6018 mL | 3.0091 mL | 6.0181 mL | |
| 10 mM | 0.3009 mL | 1.5045 mL | 3.0091 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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