SU0268
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MedKoo CAT#: 463689

CAS#: 2210228-45-6

Description: SU0268 is a potent and selective OGG1 inhibitor. DNA glycosylases involved in the first step of the DNA base excision repair pathway are promising targets in cancer therapy. There is evidence that reduction of their activities may enhance cell killing in malignant tumors.


Chemical Structure

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SU0268
CAS# 2210228-45-6

Theoretical Analysis

MedKoo Cat#: 463689
Name: SU0268
CAS#: 2210228-45-6
Chemical Formula: C26H25N3O4S
Exact Mass: 475.16
Molecular Weight: 475.563
Elemental Analysis: C, 65.67; H, 5.30; N, 8.84; O, 13.46; S, 6.74

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1350 2 Weeks
500mg USD 2350 2 Weeks
1g USD 3450 2 Weeks
2g USD 5850 2 Weeks
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Synonym: SU0268; SU 0268; SU-0268;

IUPAC/Chemical Name: 4'-(N-(1-(cyclopropanecarbonyl)-1,2,3,4-tetrahydroquinolin-7-yl)sulfamoyl)-[1,1'-biphenyl]-3-carboxamide

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)

SMILES Code: O=C(C1=CC(C2=CC=C(S(=O)(NC3=CC4=C(C=C3)CCCN4C(C5CC5)=O)=O)C=C2)=CC=C1)N

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: SU0268 is an inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1; IC50 = 0.059 µM).
In vitro activity: SU0268 is a potentially useful tool in studies of the role of OGG1 in multiple disease-related pathways. SU0268 was confirmed to bind OGG1 both in the absence and in the presence of DNA. SU0268 was selective for inhibiting OGG1 over multiple repair enzymes, including other base excision repair enzymes, and displayed no toxicity in two human cell lines at 10 μM. SU0268 inhibited OGG1 in HeLa cells, resulting in an increase in accumulation of 8-OG in DNA. Reference: J Am Chem Soc. 2018 Feb 14;140(6):2105-2114. https://pubmed.ncbi.nlm.nih.gov/29376367/
In vivo activity: SU0268 has potential as an alternative treatment for controlling severe inflammatory responses to bacterial infection. SU0268 had a favorable effect on bacterial infection in C57BL/6 wild-type mice by suppressing inflammatory responses, particularly promoting type I IFN responses. SU0268 inhibited proinflammatory responses during Pseudomonas aeruginosa infection and induced the release of type I IFN by the mitochondrial DNA-cGAS-STING-IRF3-IFN-β axis, decreasing bacterial loads and halts disease progression. Reference: J Immunol. 2020 Oct 15;205(8):2231-2242. https://pubmed.ncbi.nlm.nih.gov/32929043/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 10.0 21.03
DMSO 10.0 21.03
Ethanol 15.0 31.54

Preparing Stock Solutions

The following data is based on the product molecular weight 475.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Tanushi X, Pinna G, Vandamme M, Siberchicot C, D'Augustin O, Di Guilmi AM, Radicella JP, Castaing B, Smith R, Huet S, Leteurtre F, Campalans A. OGG1 competitive inhibitors show important off-target effects by directly inhibiting efflux pumps and disturbing mitotic progression. Front Cell Dev Biol. 2023 Feb 3;11:1124960. doi: 10.3389/fcell.2023.1124960. PMID: 36819096; PMCID: PMC9936318. 2. Tahara YK, Auld D, Ji D, Beharry AA, Kietrys AM, Wilson DL, Jimenez M, King D, Nguyen Z, Kool ET. Potent and Selective Inhibitors of 8-Oxoguanine DNA Glycosylase. J Am Chem Soc. 2018 Feb 14;140(6):2105-2114. doi: 10.1021/jacs.7b09316. Epub 2018 Feb 5. PMID: 29376367; PMCID: PMC5823510. 3. Qin S, Lin P, Wu Q, Pu Q, Zhou C, Wang B, Gao P, Wang Z, Gao A, Overby M, Yang J, Jiang J, Wilson DL, Tahara YK, Kool ET, Xia Z, Wu M. 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. doi: 10.4049/jimmunol.1901533. Epub 2020 Sep 14. PMID: 32929043; PMCID: PMC7541742.
In vitro protocol: 1. Tanushi X, Pinna G, Vandamme M, Siberchicot C, D'Augustin O, Di Guilmi AM, Radicella JP, Castaing B, Smith R, Huet S, Leteurtre F, Campalans A. OGG1 competitive inhibitors show important off-target effects by directly inhibiting efflux pumps and disturbing mitotic progression. Front Cell Dev Biol. 2023 Feb 3;11:1124960. doi: 10.3389/fcell.2023.1124960. PMID: 36819096; PMCID: PMC9936318. 2. Tahara YK, Auld D, Ji D, Beharry AA, Kietrys AM, Wilson DL, Jimenez M, King D, Nguyen Z, Kool ET. Potent and Selective Inhibitors of 8-Oxoguanine DNA Glycosylase. J Am Chem Soc. 2018 Feb 14;140(6):2105-2114. doi: 10.1021/jacs.7b09316. Epub 2018 Feb 5. PMID: 29376367; PMCID: PMC5823510.
In vivo protocol: 1. Qin S, Lin P, Wu Q, Pu Q, Zhou C, Wang B, Gao P, Wang Z, Gao A, Overby M, Yang J, Jiang J, Wilson DL, Tahara YK, Kool ET, Xia Z, Wu M. 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. doi: 10.4049/jimmunol.1901533. Epub 2020 Sep 14. PMID: 32929043; PMCID: PMC7541742.

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1: Kant M, Tahara YK, Jaruga P, Coskun E, Lloyd RS, Kool ET, Dizdaroglu M. Inhibition by Tetrahydroquinoline Sulfonamide Derivatives of the Activity of Human 8-Oxoguanine DNA Glycosylase (OGG1) for Several Products of Oxidatively induced DNA Base Lesions. ACS Chem Biol. 2020 Dec 17. doi: 10.1021/acschembio.0c00877. Epub ahead of print. PMID: 33331782.

2: Qin S, Lin P, Wu Q, Pu Q, Zhou C, Wang B, Gao P, Wang Z, Gao A, Overby M, Yang J, Jiang J, Wilson DL, Tahara YK, Kool ET, Xia Z, Wu M. 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. doi: 10.4049/jimmunol.1901533. Epub 2020 Sep 14. PMID: 32929043; PMCID: PMC7541742.

3: Tahara YK, Auld D, Ji D, Beharry AA, Kietrys AM, Wilson DL, Jimenez M, King D, Nguyen Z, Kool ET. Potent and Selective Inhibitors of 8-Oxoguanine DNA Glycosylase. J Am Chem Soc. 2018 Feb 14;140(6):2105-2114. doi: 10.1021/jacs.7b09316. Epub 2018 Feb 5. PMID: 29376367; PMCID: PMC5823510.