| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
The primary target of OGG1-IN-O8 is OGG1 (8-oxoguanine DNA glycosylase 1). It acts as a potent inhibitor of OGG1, reducing its glycosylase and lyase activities. OGG1 is responsible for targeting and removing the oxidative DNA lesion 8-oxoguanine from damaged DNA. By inhibiting OGG1, the compound impedes the repair of oxidative DNA damage.
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| ln Vitro |
OGG1-IN-08 (50 μM) suppresses various activities of DNA glycosylases, including Fpg (91.74%), endonuclease III-like (NTH1) (63.09%), and nei endonuclease VIII-like 1 DNA glycosylase (NEIL1) (84.56%)[1]. When compared to no inhibitor control, OGG1-IN-08 (10 μM) exhibits inhibitory OGG1 lyase activity on substrates containing AP sites [1]. When compared to no inhibitor, OGG1-IN-08 (10 μM) lowers the quantity of bases that OGG1 releases into solution in 8-oxo-Gua and FapyGua [1].
In vitro, OGG1-IN-O8 inhibits OGG1 with an IC50 of 0.22-0.35 µM. It reduces the glycosylase and lyase activities of OGG1. It is selective for OGG1 over NEIL1, NTH1, and Fpg at 50 µM. Its inhibitory activity is measured using enzymatic assays that monitor the removal of 8-oxoguanine from DNA. |
| ln Vivo |
In vivo, OGG1-IN-O8 has not been extensively studied in animal models. By inhibiting OGG1, it could potentially modulate the repair of oxidative DNA damage in vivo, which may have implications for cancer, neurodegeneration, and aging.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for OGG1-IN-O8 involve OGG1 inhibition assays using purified OGG1 enzyme or cell extracts. The compound's inhibitory activity is measured by monitoring the removal of 8-oxoguanine from a fluorescently labeled or radiolabeled DNA substrate. IC50 values are determined from dose-response curves. Selectivity is assessed by profiling against other DNA glycosylases.
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| Cell Assay |
In vitro cellular assays for OGG1-IN-O8 are conducted in cell lines that have been exposed to oxidative stress. Cells are treated with the compound, and the repair of oxidative DNA damage is assessed by measuring the levels of 8-oxoguanine in DNA using immunofluorescence or HPLC. The compound's effects on cell viability and DNA damage signaling are also evaluated.
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| Animal Protocol |
In vivo animal studies for OGG1-IN-O8 are not extensively documented. As a research tool for studying DNA repair, it may be used in animal models of oxidative stress or cancer. Animals would be administered the compound, and its effects on DNA damage repair, tumorigenesis, or neurodegeneration would be assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of OGG1-IN-O8 indicate it has a molecular weight of 261.13 and a molecular formula of C9H6Cl2N2OS. It is soluble in DMSO. The compound is typically stored as a powder at appropriate conditions. Its bioavailability and other PK parameters would be determined in preclinical studies.
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| Toxicity/Toxicokinetics |
Toxicological information for OGG1-IN-O8 is limited to its use as a research chemical. As a DNA repair inhibitor, it may increase the accumulation of oxidative DNA damage, leading to mutagenesis and genomic instability. Comprehensive toxicology studies would be required for its use in vivo.
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| References |
[1]. Nathan Donley,et al. Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1). ACS Chem Biol. 2015 Oct 16;10(10):2334-43.
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| Additional Infomation |
OGG1-IN-O8 is a research compound used as a potent and selective inhibitor of OGG1. It is also known as OGG1-IN-08. It is used to study the role of OGG1 in DNA repair and its implications in cancer, neurodegeneration, and aging. It is available from research chemical suppliers for preclinical studies. It is not approved for clinical use.
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| Molecular Formula |
C9H6CL2N2OS
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|---|---|
| Molecular Weight |
261.12
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| Exact Mass |
259.957
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| CAS # |
350997-39-6
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| Related CAS # |
350997-39-6;
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| PubChem CID |
874733
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.718
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| LogP |
2.34
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
15
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| Complexity |
267
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NNC(C1SC2=CC=CC(Cl)=C2C=1Cl)=O
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| InChi Key |
HSSHUDKWJRJKPV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H6Cl2N2OS/c10-4-2-1-3-5-6(4)7(11)8(15-5)9(14)13-12/h1-3H,12H2,(H,13,14)
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| Chemical Name |
3,4-dichloro-1-benzothiophene-2-carbohydrazide
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| Synonyms |
OGG1INO8; OGG1 IN O8; OGG1-IN-O8
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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 : ~25 mg/mL (~95.74 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 | 3.8297 mL | 19.1483 mL | 38.2966 mL | |
| 5 mM | 0.7659 mL | 3.8297 mL | 7.6593 mL | |
| 10 mM | 0.3830 mL | 1.9148 mL | 3.8297 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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