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SU-0268 (SU0268)

Alias: SU0268; SU-0268; SU 0268
Cat No.:V41507 Purity: ≥98%
SU-0268 (SU0268) is a selective OGG1 (8-Oxoguanine DNA glycosylase 1) inhibitor involved in the regulation of inflammatory responses during Pseudomonas aeruginosa infection.
SU-0268 (SU0268)
SU-0268 (SU0268) Chemical Structure CAS No.: 2210228-45-6
Product category: OGG1
This product is for research use only, not for human use. We do not sell to patients.
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Product Description

SU-0268 (SU0268) is a selective OGG1 (8-Oxoguanine DNA glycosylase 1) inhibitor involved in the regulation of inflammatory responses during Pseudomonas aeruginosa infection.

Biological Activity I Assay Protocols (From Reference)
Targets
OGG1 ( IC50 = 0.059 μM )
ln Vitro
IACS-4759 and SU0268 co-treated cells (5–20 μM, 48 hours) outperformed IACS treated in the same way [1]. More viable cells are those treated with SU0268 or -4759 [1]. reacts to OGG1 oscillations rather than its substrate since it does not bind DNA [2]. SU0268 reduces obesity and stops the course of disease by inducing the release of type I interferons along the DNA-cGAS-STING-IRF3-IFN-β axis [3].
ln Vivo
SU0268 grooming (10 mg/kg, intranasal therapy) enhanced the mortality of MH-S cells and C57BL/6N mice compared with pregnancies without SU0268 grooming [3].
Cell Assay
Cell viability assay [1]
Cell Types: A549 shGFP and shMTH1 (2000 cells per well).
Tested Concentrations: 0.1μM, 0.5μM, 1μM, 2.5μM, 5μM, 7.5μM, 10μM.
Incubation Duration: 24 or 48 hrs (hours).
Experimental Results: shGFP cells were more susceptible to OGG1 inhibition by increasing SU0268 doses than shMTH1 cells, especially at the 48 time point.
Animal Protocol
Animal/Disease Models: Anesthetize C57BL/ 6N mice [3].
Doses: 10 mg/kg.
Route of Administration: Intranasal treatment.
Experimental Results: Dramatically inhibited inflammatory response and alleviated Pseudomonas aeruginosa infection.
References

[1]. OGG1 co-inhibition antagonizes the tumor-inhibitory effects of targeting MTH1. Redox Biol. 2021 Apr;40:101848.

[2]. Potent and Selective Inhibitors of 8-Oxoguanine DNA Glycosylase. J Am Chem Soc. 2018 Feb 14;140(6):2105-2114.

[3]. Small-Molecule Inhibitor of 8-Oxoguanine DNA Glycosylase 1 Regulates Inflammatory Responses during Pseudomonas aeruginosa Infection. J Immunol. 2020 Oct 15;205(8):2231-2242.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H25N3O4S
Molecular Weight
475.5594
Exact Mass
475.16
Elemental Analysis
C, 65.67; H, 5.30; N, 8.84; O, 13.46; S, 6.74
CAS #
2210228-45-6
PubChem CID
154934526
Appearance
White to off-white solid powder
LogP
3.2
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
6
Heavy Atom Count
34
Complexity
860
Defined Atom Stereocenter Count
0
InChi Key
XGGNCZLDTJOSFV-UHFFFAOYSA-N
InChi Code
InChI=1S/C26H25N3O4S/c27-25(30)21-4-1-3-20(15-21)17-9-12-23(13-10-17)34(32,33)28-22-11-8-18-5-2-14-29(24(18)16-22)26(31)19-6-7-19/h1,3-4,8-13,15-16,19,28H,2,5-7,14H2,(H2,27,30)
Chemical Name
3-[4-[[1-(cyclopropanecarbonyl)-3,4-dihydro-2H-quinolin-7-yl]sulfamoyl]phenyl]benzamide
Synonyms
SU0268; SU-0268; SU 0268
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO: 95~100 mg/mL (199.8~210.3 mM)
Ethanol: 2 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.26 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 25.0 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: ≥ 2.5 mg/mL (5.26 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 25.0 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1028 mL 10.5139 mL 21.0278 mL
5 mM 0.4206 mL 2.1028 mL 4.2056 mL
10 mM 0.2103 mL 1.0514 mL 2.1028 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • The OGG1-specific small molecule inhibitor, SU0268, is less effective in shMTH1-transduced cells vs. control shGFP-transduced cells. Redox Biol . 2021 Apr:40:101848.
  • SU0268 promotes mtDNA release into the cytoplasm after ROS-induced DNA damage in response to P. aeruginosa infection. J Immunol . 2020 Oct 15;205(8):2231-2242.
  • SU0268 promotes mtDNA release dependent on the BAK/BAX axis. J Immunol . 2020 Oct 15;205(8):2231-2242.
  • Synthesis of the OGG1 Inhibitor SU0268 (41). J Am Chem Soc . 2018 Feb 14;140(6):2105-2114.
  • SU0268 (41) specifically binds OGG1. 3000 RU (resonance units) of recombinant biotinylated OGG1 was immobilized onto streptavidin sensor chip SA, and experiments were performed on a Biacore 8K with a 1:3 dilution series of inhibitor 41 (highest concentration 4 μM) (a) Sensorgram plots of inhibitor 41. J Am Chem Soc . 2018 Feb 14;140(6):2105-2114.
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