| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Glyoxalase I inhibitor 6 targets Glyoxalase I (Glo-I), an enzyme that detoxifies methylglyoxal. By inhibiting Glo-I, the compound leads to the accumulation of methylglyoxal, inducing cytotoxic stress in cancer cells.
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|---|---|
| ln Vitro |
In vitro enzyme assays confirm that Glyoxalase I inhibitor 6 has an IC50 of 1.13 microM against Glo-I. It is particularly noted for its potential as an anticancer agent with low toxicity, suggesting a therapeutic window for selectively targeting cancer cells over normal cells.
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| ln Vivo |
Dedicated in vivo efficacy studies for inhibitor 6 are not extensively documented in standard profiles. However, due to its low toxicity profile, it may be better suited for in vivo applications compared to other Glo-I inhibitors. Further animal studies are required to confirm efficacy.
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| Enzyme Assay |
Recombinant human Glyoxalase I is incubated with methylglyoxal and glutathione. The enzymatic activity is measured spectrophotometrically by detecting the formation of S-D-lactoylglutathione at 240 nm in the presence of varying concentrations of Glyoxalase I inhibitor 6.
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| Cell Assay |
Normal and cancer cell lines are cultured and treated with Glyoxalase I inhibitor 6. Cell viability is assessed using MTT or CCK-8 assays. The concentration causing 50% growth inhibition (GI50) is calculated, and selectivity for cancer over normal cells is determined to assess its low toxicity claim.
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| Animal Protocol |
In vivo protocols would typically involve establishing xenograft tumors in mice. The compound would be administered intraperitoneally or orally. Tumor growth inhibition would be monitored, and body weight would be recorded as an indicator of systemic toxicity.
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| ADME/Pharmacokinetics |
Detailed PK parameters for Glyoxalase I inhibitor 6 are not extensively documented. As a research compound with an IC50 in the low micromolar range, extensive ADME profiling has not been publicly reported. It is typically used in cellular and initial in vivo studies.
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| Toxicity/Toxicokinetics |
The most notable feature of Glyoxalase I inhibitor 6 is its low toxicity profile. While detailed toxicological studies are not reported, the compound is described as having low toxicity, suggesting it is well-tolerated in preliminary evaluations. Standard lab precautions still apply.
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| References | |
| Additional Infomation |
Glyoxalase I inhibitor 6 is designated as Compound 9j. It is a more advanced analog in a series of Glo-I inhibitors. The low toxicity feature distinguishes it from inhibitor 5 and other compounds, potentially offering a better therapeutic window for in vivo cancer models.
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| Molecular Formula |
C18H15N3O5S
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|---|---|
| Molecular Weight |
385.393802881241
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| Exact Mass |
385.073
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| CAS # |
2455508-19-5
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| PubChem CID |
162652988
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| Appearance |
Light brown to brown solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
677
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(O)=C2C(C=CC=C2)=C(/N=N/C2=CC=C(C)C(S(N)(=O)=O)=C2)C=C1C(O)=O
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| InChi Key |
DXHDPHYZULAOTP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15N3O5S/c1-10-6-7-11(8-16(10)27(19,25)26)20-21-15-9-14(18(23)24)17(22)13-5-3-2-4-12(13)15/h2-9,22H,1H3,(H,23,24)(H2,19,25,26)
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| Chemical Name |
1-hydroxy-4-[(4-methyl-3-sulfamoylphenyl)diazenyl]naphthalene-2-carboxylic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.5948 mL | 12.9739 mL | 25.9477 mL | |
| 5 mM | 0.5190 mL | 2.5948 mL | 5.1895 mL | |
| 10 mM | 0.2595 mL | 1.2974 mL | 2.5948 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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