PeptideDB

SU-0268 (SU0268) 2210228-45-6

SU-0268 (SU0268) 2210228-45-6

CAS No.: 2210228-45-6

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



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)

Biological Activity


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.


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.

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.