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| Targets |
L82-G17 specifically targets DNA ligase I (Lig I). This enzyme catalyzes the joining of Okazaki fragments during DNA replication and is also involved in various DNA repair pathways. As a non-competitive inhibitor, L82-G17 binds to a site other than the enzyme's active site, preventing the formation of phosphodiester bonds in the final step of the ligation reaction.
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| ln Vitro |
LigI is selectively and uncompetitively inhibited by L82-G17 (200 μM, 30 min)[1]. LigI binding to non-ligatable nicked DNA binding is enhanced by L82-G17 (0-100 μM)[1]. Step 3 of the ligation procedure, the creation of phosphodiester bonds, is inhibited by L82-G17[1]. L82-G17 (0-100 μM) causes damage to DNA and prevents cell viability and DNA synthesis[1].
In vitro, L82-G17 selectively inhibits DNA ligase I activity. It acts as a non-competitive inhibitor, which means it does not compete with the DNA substrate for binding. By preventing the creation of phosphodiester bonds, it blocks the third and final stage of the ligation reaction, thereby inhibiting the completion of DNA replication and repair processes. |
| ln Vivo |
In vivo data for L82-G17 is not extensively reported in publicly available sources. As a selective DNA ligase I inhibitor, the compound has potential applications in animal models of cancer, where inhibiting DNA repair could sensitize tumors to DNA-damaging agents. However, specific published in vivo efficacy studies are not detailed in the current literature. L82-G17 is primarily used as a research tool for studying DNA replication and repair mechanisms.
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| Enzyme Assay |
The in vitro DNA ligase I inhibition assay for L82-G17 uses purified DNA ligase I enzyme and a nicked DNA substrate. Enzyme activity is measured by monitoring the ligation of the DNA strands, typically using gel electrophoresis or fluorescence-based methods. IC50 values are calculated from dose-response curves. The compound's non-competitive mechanism is confirmed by performing the assay at different substrate concentrations.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HeLa cells Tested Concentrations: 0-30 μM Incubation Duration: 5 days Experimental Results: decreased cell number by about 70% at 20 μM. Cell Proliferation Assay[1] Cell Types: CH12F3 WT and CH12F3Δ/Δ cells Tested Concentrations: 0-100 μM Incubation Duration: 72 h Experimental Results: Had great effect on the proliferation and survival of the parental CH12F3 cells. Cellular assays for L82-G17 are conducted in cancer cell lines where DNA ligase I is active. Cells are treated with varying concentrations of the compound, and the effects on DNA replication and repair are assessed by measuring cell proliferation, DNA synthesis, or the accumulation of DNA damage markers. The compound's selectivity for DNA ligase I over other ligases is confirmed in cell-based models. |
| Animal Protocol |
In vivo studies for L82-G17 would typically involve xenograft mouse models of cancer. The compound would be administered via intraperitoneal or intravenous routes at doses determined by pharmacokinetic studies, potentially in combination with DNA-damaging chemotherapies. Efficacy would be assessed by measuring tumor growth inhibition and DNA damage in tumor tissues. However, specific published in vivo protocols for L82-G17 are not available.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for L82-G17 is not extensively reported in publicly available sources. As a small molecule inhibitor, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life, bioavailability, and clearance have not been reported in the available literature. Researchers interested in the pharmacokinetic properties of L82-G17 should consult the original research articles or contact the manufacturer.
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| Toxicity/Toxicokinetics |
Toxicity data for L82-G17 is not publicly available. As a research compound, its safety profile would typically be evaluated in in vitro cytotoxicity assays and in vivo tolerability studies. However, specific toxicity data has not been reported in the available literature. As with all research compounds, L82-G17 is intended for research use only and not for human therapeutic applications.
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| References | |
| Additional Infomation |
L82-G17 (CAS 92285-87-5) is a non-competitive and selective inhibitor of DNA ligase I. It functions by preventing the creation of phosphodiester bonds, the third stage of the ligation reaction. This makes it a valuable tool for studying DNA replication, repair pathways, and for cancer research where DNA ligase I is a therapeutic target. Further information on this compound would require access to specialized chemical databases or the original literature.
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| Molecular Formula |
C11H9CLN4O2
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| Molecular Weight |
264.67
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| Exact Mass |
264.041
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| Elemental Analysis |
C, 49.92; H, 3.43; Cl, 13.39; N, 21.17; O, 12.09
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| CAS # |
92285-87-5
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| PubChem CID |
5711175
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| Appearance |
Pink to orange solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.685
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| LogP |
0.99
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
419
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C(NN=CC=1N/N=C\C1C=CC=C(C=1)O)=O
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| InChi Key |
PYYWVUBALUMAIY-WLRTZDKTSA-N
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| InChi Code |
InChI=1S/C11H9ClN4O2/c12-10-9(6-14-16-11(10)18)15-13-5-7-2-1-3-8(17)4-7/h1-6,17H,(H2,15,16,18)/b13-5+
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| Chemical Name |
5-chloro-4-[(2E)-2-[(3-hydroxyphenyl)methylidene]hydrazinyl]-1H-pyridazin-6-one
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| Synonyms |
L82-G17; L82 G17; L82G17
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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 : ~125 mg/mL (~472.3 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7783 mL | 18.8914 mL | 37.7829 mL | |
| 5 mM | 0.7557 mL | 3.7783 mL | 7.5566 mL | |
| 10 mM | 0.3778 mL | 1.8891 mL | 3.7783 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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